Daporinad (Synonyms: 達(dá)珀利奈; FK866; APO866)

目錄號(hào): HY-50876 純度: 99.72%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Daporinad (FK866) 是煙酰胺磷酸核糖轉(zhuǎn)移酶 (NMPRTase; Nampt) 的有效抑制劑， IC₅₀ 為 0.09 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Daporinad Chemical Structure

CAS No. : 658084-64-1

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥729	In-stock
5 mg	￥663	In-stock
10 mg	￥1252	In-stock
25 mg	￥1950	In-stock
50 mg	￥2950	In-stock
100 mg	￥4400	In-stock
200 mg		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

Other Forms of Daporinad:

(E/Z)-Daporinad hydrochloride 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻(xiàn)

•Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X. [Abstract]
•Cell Death Differ. 2024 Jan 5. [Abstract]
•Redox Biol. 2024 Jan 3:69:103030. [Abstract]
•Sci Adv. 2023 Apr 14;9(15):eadf8522. [Abstract]
•Hepatology. 2022 Jul 11. [Abstract]
•Cell Chem Biol. 2024 May 20:S2451-9456(24)00179-X. [Abstract]

•Acta Pharmacol Sin. 2023 Jun 5. [Abstract]
•Acta Pharmacol Sin. 2023 Apr 25.
•Biochim Biophys Acta Mol Basis Dis. 2024 Jun 9:167288. [Abstract]
•J Agric Food Chem. 2024 Apr 15. [Abstract]
•Sci Signal. 2021 Jun 8;14(686):eabc7405. [Abstract]
•PLoS Pathog. 2021 Mar 19;17(3):e1009436. [Abstract]
•Mol Carcinog. 2024 Sep 10. [Abstract]
•Front Cell Dev Biol. 2022 Mar 24:10:853652. [Abstract]
•J Cell Physiol. 2023 Nov 22. [Abstract]
•Cells. 2023 Oct 2, 12(19), 2396.
•Int Immunopharmacol. 2023 May 12;120:110291. [Abstract]
•Cancers (Basel). 2023 Apr 23, 15(9), 2427.
•Sci Rep. 2023 Feb 27;13(1):3334. [Abstract]
•Mol Neurobiol. 2022 Nov 28. [Abstract]
•Molecules. 2022 Mar 21;27(6):2011. [Abstract]
•Front Pharmacol. 2020 Jul 29;11:1136. [Abstract]
•J Cell Physiol. 2019 Apr;234(4):4385-4395. [Abstract]
•Brain Res Bull. 2024 Nov 1:218:111114. [Abstract]
•Neurosci Lett. 2023 Sep 4;137471. [Abstract]
•J Biol Chem. 2022 Oct 12;102587. [Abstract]
•Genes Genomics. 2022 Oct 10. [Abstract]
•Cancer Manag Res. 2021 Nov 30;13:8915-8928. [Abstract]
•PeerJ. 2021 May 14;9:e11401. [Abstract]
•Pancreatology. 2021 Mar 25.
•Mol Med Rep. 2017 Oct;16(4):5121-5128. [Abstract]
•Rapid Commun Mass Spectrom. 2021 Sep 30;35(18):e9150. [Abstract]
•bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
•Research Square Preprint. 2024 Apr 12.
•Research Square Preprint. 2024 Mar 6.
•Research Square Preprint. 2023 Nov 14.
•Research Square Preprint. 2023 Sep 8.
•bioRxiv. 2019 Oct 28.
•bioRxiv. 2019 Oct.
•Patent. US20180263995A1.

: Daporinad purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Apr;234(4):4385-4395. [Abstract]; SW620 and HCT116 cells are seeded into a six-well plate for 72 hr, followed by treatment with different concentrations (100 nM and 10 μM) of FK866 for 24 hr.

: Daporinad purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Oct;16(4):5121-5128. [Abstract]; Effects of Emodin, FK866 and DEX on PMN apoptosis in SAP rats. Protein expression levels of Fas, FasL, Bax, cleaved caspase 3 and Bcl xL are detected by western blotting. β actin served as an internal control. Data are presented as the mean±standard deviation.

Daporinad 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC₅₀ of 0.09 nM.

IC₅₀ & Target

IC50: 0.09 nM (NMPRTase)

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.001 μM Compound: 8; APO866	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.001 μM Compound: 1, APO866	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay Cytotoxicity against human A2780 cells after 72 hrs by SRB assay	[PMID: 23617784]
A2780	IC₅₀	0.001 μM Compound: 2, APO-866, FK866	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay	[PMID: 24405419]
A2780	IC₅₀	0.001 μM Compound: 2, APO-866	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
A2780	IC₅₀	1.6 nM Compound: 1, APO866	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
A2780	IC₅₀	5.7 nM Compound: 1, APO866	Cytotoxicity against human A2780 cells by clonogenic assay Cytotoxicity against human A2780 cells by clonogenic assay	[PMID: 24164086]
A-431	IC₅₀	6.1 nM Compound: 1, APO866	Cytotoxicity against human A431 cells by clonogenic assay Cytotoxicity against human A431 cells by clonogenic assay	[PMID: 24164086]
A549	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human A549 cells after 6 days by SRB assay Cytotoxicity against human A549 cells after 6 days by SRB assay	[PMID: 21330015]
A549	IC₅₀	0.028 μM Compound: 1; FK866; AP0866	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by cell titer glo luminescent assay	[PMID: 35640078]
A549	IC₅₀	3.7 μM Compound: FK866	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
DU-145	IC₅₀	5.12 nM Compound: FK866, APO866; 1	Antiproliferative activity against human DU145 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human DU145 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
HCT-116	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human HCT116 cells after 6 days by SRB assay Cytotoxicity against human HCT116 cells after 6 days by SRB assay	[PMID: 21330015]
HCT-116	IC₅₀	1.6 μM Compound: FK866	Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
HCT-116	IC₅₀	1.6 μM Compound: 2; FK228	Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
HCT-116	IC₅₀	10.9 nM Compound: 1, APO866	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
HCT-116	IC₅₀	946 nM Compound: 1, APO866	Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
HeLa	GI₅₀	1.34 nM Compound: 1; APO-866; FK866	Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
HeLa	IC₅₀	3.75 nM Compound: FK866, APO866; 1	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
HepG2	IC₅₀	0.89 μM Compound: FK866	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 29348808]
HepG2	IC₅₀	0.89 μM Compound: 2; FK228	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
HepG2	IC₅₀	18.72 nM Compound: 1; FK866	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 31818629]
HepG2	IC₅₀	2.2 nM Compound: 1, APO866	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis	[PMID: 24164086]
HT-1080	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human HT1080 cells after 6 days by SRB assay Cytotoxicity against human HT1080 cells after 6 days by SRB assay	[PMID: 21330015]
Huh-7	IC₅₀	1.05 nM Compound: FK866, APO866; 1	Antiproliferative activity against human HuH7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human HuH7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
K562	IC₅₀	> 20 μM Compound: 1, FK-866	Cytotoxicity against human K562 cells after 6 days by SRB assay Cytotoxicity against human K562 cells after 6 days by SRB assay	[PMID: 21330015]
K562	IC₅₀	0.96 nM Compound: FK866, APO866; 1	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
K562	IC₅₀	7.2 nM Compound: 1, FK866, WK175, APO866	Cytotoxicity against human K562 cells after 96 hrs by MTT assay Cytotoxicity against human K562 cells after 96 hrs by MTT assay	[PMID: 23679915]
MCF7	GI₅₀	0.29 nM Compound: 1; APO-866; FK866	Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
MCF7	IC₅₀	0.41 nM Compound: FK866, APO866; 1	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
MCF7	IC₅₀	0.68 μM Compound: 1, FK-866	Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay	[PMID: 21330015]
MCF7	IC₅₀	7.4 nM Compound: 1, APO866	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
MCF7	IC₅₀	8.4 nM Compound: 1, APO866	Cytotoxicity against human MCF7 cells by clonogenic assay Cytotoxicity against human MCF7 cells by clonogenic assay	[PMID: 24164086]
MDA-MB-231	GI₅₀	0.78 nM Compound: 1; APO-866; FK866	Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
MDA-MB-231	IC₅₀	1.3 μM Compound: 2; FK228	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28885834]
NCI-H1975	GI₅₀	3.95 nM Compound: 1; APO-866; FK866	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]
NCI-H1975	IC₅₀	4.76 nM Compound: FK866, APO866; 1	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutation assessed as inhibition of cell growth after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutation assessed as inhibition of cell growth after 72 hrs by CCK-8 assay	[PMID: 30992165]
PC-3	IC₅₀	0.006 μM Compound: 4; FK866	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by Celltiter-Glo assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by Celltiter-Glo assay	[PMID: 31303996]
PC-3	IC₅₀	3.8 nM Compound: 1, APO866	Cytotoxicity against human PC3 cells by clonogenic assay Cytotoxicity against human PC3 cells by clonogenic assay	[PMID: 24164086]
PC-3	IC₅₀	5.7 nM Compound: 1; FK866	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay	[PMID: 28610984]
SH-SY5Y	IC₅₀	1.7 nM Compound: 1, FK-866, APO-866	Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 19961183]
SH-SY5Y	EC₅₀	2.5 nM Compound: 4; FK866	Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells measured after 48 hrs by MTT assay	[PMID: 31400709]
SH-SY5Y	EC₅₀	3.2 nM Compound: FK866	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00261C
SH-SY5Y	EC₅₀	3.4 nM Compound: 1; FK866	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay	[PMID: 28165742]
SH-SY5Y	IC₅₀	30.1 pM Compound: FK866	Inhibition of NAMPT in human SH-SY5Y cells assessed as NAD depletion incubated for 16 hrs Inhibition of NAMPT in human SH-SY5Y cells assessed as NAD depletion incubated for 16 hrs	10.1039/C5MD00261C
SK-OV-3	IC₅₀	211 nM Compound: 1, APO866	Cytotoxicity against human SKOV3 cells by clonogenic assay Cytotoxicity against human SKOV3 cells by clonogenic assay	[PMID: 24164086]
SNU-638	IC₅₀	< 0.16 μM Compound: 1, FK-866	Cytotoxicity against human SNU638 cells after 6 days by SRB assay Cytotoxicity against human SNU638 cells after 6 days by SRB assay	[PMID: 21330015]
U-937	GI₅₀	0.36 nM Compound: 1; APO-866; FK866	Cytotoxicity against human U937 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay Cytotoxicity against human U937 cells assessed as cell growth inhibition after 72 hrs by CCK-8 assay	[PMID: 27224875]

體外研究
(In Vitro)

使用 (E)-Daporinad 抑制 Nampt 可誘導(dǎo)細(xì)胞內(nèi) NAD⁺ 顯著減少并選擇性殺死 MM 細(xì)胞。(E)-Daporinad 誘導(dǎo)的細(xì)胞死亡與 Nampt 活性抑制有關(guān)，而非蛋白質(zhì)表達(dá)，并且 MM 細(xì)胞中 NAD⁺ 基線水平高于正常 PBMC，這賦予了 (E)-Daporinad 敏感性。 (E)-Daporinad 消除了骨髓微環(huán)境賦予的生存優(yōu)勢(shì)^[1]。 (E)-Daporinad 可防止不同絲裂原誘導(dǎo)的 [Ca²⁺]i 升高，并降低 Jurkat 和活化的 PBL 中 TG 反應(yīng)性 Ca²⁺ 庫(kù)的 Ca²⁺ 含量。(E)-Daporinad 可降低 Jurkat 細(xì)胞中 TG 反應(yīng)性 Ca²⁺ 庫(kù)的 Ca²⁺ 含量，但不會(huì)降低 Bcl2-Jurkat 細(xì)胞中的 TG 反應(yīng)性 Ca²⁺ 含量^[2]。 (E)-Daporinad 抑制 NAMPT 或煙酰胺抑制 SIRT 可降低涉及 p53 乙酰化途徑的 293T 細(xì)胞增殖并引發(fā)其死亡^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

(E)-Daporinad (FK866) (30 mg/kg，腹腔注射) 降低 CB17-SCID 小鼠的腫瘤負(fù)擔(dān)，腫瘤組織中 ERK 磷酸化和 LC3^[1] 蛋白水解酶裂解顯著減少。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

391.51

Formula

C₂₄H₂₉N₃O₂

CAS 號(hào)

658084-64-1

性狀

固體

顏色

White to light yellow

中文名稱

達(dá)珀利奈

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 50 mg/mL (127.71 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5542 mL	12.7711 mL	25.5421 mL
5 mM	0.5108 mL	2.5542 mL	5.1084 mL
10 mM	0.2554 mL	1.2771 mL	2.5542 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.39 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

方案一

請(qǐng)依序添加每種溶劑： 50% PEG300 50% Saline
Solubility: 5 mg/mL (12.77 mM); 澄清溶液; 超聲助溶
方案二

請(qǐng)依序添加每種溶劑： 20% SBE-β-CD in Saline
Solubility: 4 mg/mL (10.22 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.91%

選擇批次：

Data Sheet (642 KB) SDS (393 KB)

COA (281 KB) HNMR (223 KB) LCMS (402 KB) 元素分析報(bào)告 (204 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29. [Content Brief]

[2]. Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81. [Content Brief]

[3]. Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7. [Content Brief]

Cell Assay ^[1]	MM1S cells (2×10⁴?cells/well) are cultured for 72 and 96 hours in BMSC-coated 96-well plates in the presence or absence of drug. DNA synthesis is measured by (³H)-thymidine uptake, with (³H)-thymidine added (0.5 μCi/well) during the last 8 hours of cultures. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3×10⁶?MM1S cells in 100 μL RPMI 1640. After detection of tumor (2 weeks after the injection), 7 mice are treated intraperitoneally with either vehicle or (E)-Daporinad (FK866) (30 mg/kg body weight) twice a day for 4 days, repeated weekly over 3 weeks. Caliper measurements of the longest perpendicular tumor diameters are performed twice a week to estimate the tumor volume using the following formula: length×width²×0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm³?or the mice appear moribund. Survival is evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)	[1]. Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29. [Content Brief] [2]. Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81. [Content Brief] [3]. Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7. [Content Brief]

Daporinad 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5542 mL	12.7711 mL	25.5421 mL	63.8553 mL
	5 mM	0.5108 mL	2.5542 mL	5.1084 mL	12.7711 mL
	10 mM	0.2554 mL	1.2771 mL	2.5542 mL	6.3855 mL
	15 mM	0.1703 mL	0.8514 mL	1.7028 mL	4.2570 mL
	20 mM	0.1277 mL	0.6386 mL	1.2771 mL	3.1928 mL
	25 mM	0.1022 mL	0.5108 mL	1.0217 mL	2.5542 mL
	30 mM	0.0851 mL	0.4257 mL	0.8514 mL	2.1285 mL
	40 mM	0.0639 mL	0.3193 mL	0.6386 mL	1.5964 mL
	50 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2771 mL
	60 mM	0.0426 mL	0.2129 mL	0.4257 mL	1.0643 mL
	80 mM	0.0319 mL	0.1596 mL	0.3193 mL	0.7982 mL
	100 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6386 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Daporinad (Synonyms: 達(dá)珀利奈; FK866; APO866)

Customer Review

Other Forms of Daporinad:

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻(xiàn)

Daporinad 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Daporinad 相關(guān)分類

完整儲(chǔ)備液配制表

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Daporinad (Synonyms: 達(dá)珀利奈; FK866; APO866)

Customer Review

Other Forms of Daporinad:

Daporinad 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻(xiàn)

Daporinad 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

Daporinad 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Daporinad 相關(guān)分類

完整儲(chǔ)備液配制表

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