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  2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. GNE-6468

GNE-6468 是一個(gè)有效且有選擇性的 RORγ (RORc) 反向激動(dòng)劑，EC50 值為 2 nM。GNE-6468 抑制 PBMC 中 IL-17 的 EC50 值為 30 nM。

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GNE-6468 Chemical Structure

GNE-6468 Chemical Structure

CAS No. : 1677668-27-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4180
In-stock
1 mg ￥1600
In-stock
5 mg ￥3800
In-stock
10 mg 現(xiàn)貨 詢(xún)價(jià)
50 mg   詢(xún)價(jià)  
100 mg   詢(xún)價(jià)  

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Customer Review

查看 ROR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC[1].

IC50 & Target[1]

ROR-γ

2 nM (EC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
0.013 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
PBMC EC50
> 10 μM
Compound: 28, GNE-6468
Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay
[PMID: 26048793]
PBMC EC50
> 10 μM
Compound: 28, GNE-6468
Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA
Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA
[PMID: 26048793]
PBMC EC50
0.03 μM
Compound: 28, GNE-6468
Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA
[PMID: 26048793]
體內(nèi)研究
(In Vivo)

GNE-6468 (compound 28) displays high predicted clearance values in human and rodent hepatocytes (CLhep = 17 and 42 mL/min/kg, respectively) [1].

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

433.84

Formula

C23H16ClN3O4
CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

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 : 5 mg/mL (11.52 mM; 超聲助溶; 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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3050 mL 11.5250 mL 23.0500 mL
5 mM 0.4610 mL 2.3050 mL 4.6100 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)

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

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

g

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
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3050 mL 11.5250 mL 23.0500 mL 57.6249 mL
5 mM 0.4610 mL 2.3050 mL 4.6100 mL 11.5250 mL
10 mM 0.2305 mL 1.1525 mL 2.3050 mL 5.7625 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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產(chǎn)品名稱(chēng)：
GNE-6468
目錄號(hào)：
HY-19775
需求量：