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  1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Ayanin

Ayanin 是從 Psychotria serpens 中分離得到的一種具有生物學(xué)活性的黃酮類物質(zhì)。Ayanin 是非選擇性的磷酸二酯酶 (phosphodiesterase1-4) 抑制劑,可用于呼吸道疾病的研究,如過敏性哮喘等。

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)

Ayanin Chemical Structure

Ayanin Chemical Structure

CAS No. : 572-32-7

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3.  試用裝只面向終端客戶。

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查看 Phosphodiesterase (PDE) 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

Ayanin is a bioflavonoid isolated from Psychotria serpens. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al[1].

IC50 & Target[1]

PDE2A

 

PDE4

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
2008 IC50
50 μM
Compound: 16
Inhibition of MRP1 expressed in human 2008 cells assessed as calcein AM accumulation by cell based assay
Inhibition of MRP1 expressed in human 2008 cells assessed as calcein AM accumulation by cell based assay
[PMID: 21354800]
A2780 ADR IC50
9.4 μM
Compound: 16
Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
[PMID: 21354800]
A549 IC50
20.79 μM
Compound: 6a
Anticancer activity against human A549 cells by HTS assay
Anticancer activity against human A549 cells by HTS assay
[PMID: 25139569]
Calu-1 IC50
> 50 μM
Compound: 6a
Anticancer activity against human Calu1 cells by HTS assay
Anticancer activity against human Calu1 cells by HTS assay
[PMID: 25139569]
HeLa IC50
19.47 μM
Compound: 6a
Anticancer activity against human HeLa cells by HTS assay
Anticancer activity against human HeLa cells by HTS assay
[PMID: 25139569]
HOP-62 IC50
20.06 μM
Compound: 6a
Anticancer activity against human HOP62 cells by HTS assay
Anticancer activity against human HOP62 cells by HTS assay
[PMID: 25139569]
LOX IMVI IC50
45.97 μM
Compound: 6a
Anticancer activity against human LOXIMVI cells by HTS assay
Anticancer activity against human LOXIMVI cells by HTS assay
[PMID: 25139569]
M14 IC50
37.07 μM
Compound: 6a
Anticancer activity against human M14 cells by HTS assay
Anticancer activity against human M14 cells by HTS assay
[PMID: 25139569]
MCF7 IC50
0.68 μM
Compound: 16
Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
[PMID: 21354800]
MDCK IC50
0.46 μM
Compound: 16
Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
[PMID: 21354800]
MDCK IC50
13 μM
Compound: 16
Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
[PMID: 21354800]
NCI-H1299 IC50
> 50 μM
Compound: 6a
Anticancer activity against human H1299 cells by HTS assay
Anticancer activity against human H1299 cells by HTS assay
[PMID: 25139569]
NCI-H157 IC50
18.64 μM
Compound: 6a
Anticancer activity against human NCI-H157 cells by HTS assay
Anticancer activity against human NCI-H157 cells by HTS assay
[PMID: 25139569]
NCI-H1792 IC50
> 50 μM
Compound: 6a
Anticancer activity against human NCI-H1792 cells by HTS assay
Anticancer activity against human NCI-H1792 cells by HTS assay
[PMID: 25139569]
NCI-H1944 IC50
21.92 μM
Compound: 6a
Anticancer activity against human NCI-H1944 cells by HTS assay
Anticancer activity against human NCI-H1944 cells by HTS assay
[PMID: 25139569]
NCI-H460 IC50
12.79 μM
Compound: 6a
Anticancer activity against human H460 cells by HTS assay
Anticancer activity against human H460 cells by HTS assay
[PMID: 25139569]
NCI-H460 IC50
5.7 μM
Compound: 9
Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C
Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C
[PMID: 21275386]
NCI-H522 IC50
20.21 μM
Compound: 6a
Anticancer activity against human NCI-H522 cells by HTS assay
Anticancer activity against human NCI-H522 cells by HTS assay
[PMID: 25139569]
體外研究
(In Vitro)

Ayanin inhibits interleukin (IL)-4 production from purified basophils with an IC50 value of 2.2 μM[1].

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

分子量

344.32

Formula

C18H16O7

CAS 號(hào)
性狀

固體

顏色

White to yellow

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 250 mg/mL (726.07 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 2.9043 mL 14.5214 mL 29.0428 mL
5 mM 0.5809 mL 2.9043 mL 5.8085 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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.04 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 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。
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

由于實(shí)驗(yàn)過程有損耗,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 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國技術(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
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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 2.9043 mL 14.5214 mL 29.0428 mL 72.6069 mL
5 mM 0.5809 mL 2.9043 mL 5.8086 mL 14.5214 mL
10 mM 0.2904 mL 1.4521 mL 2.9043 mL 7.2607 mL
15 mM 0.1936 mL 0.9681 mL 1.9362 mL 4.8405 mL
20 mM 0.1452 mL 0.7261 mL 1.4521 mL 3.6303 mL
25 mM 0.1162 mL 0.5809 mL 1.1617 mL 2.9043 mL
30 mM 0.0968 mL 0.4840 mL 0.9681 mL 2.4202 mL
40 mM 0.0726 mL 0.3630 mL 0.7261 mL 1.8152 mL
50 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.4521 mL
60 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2101 mL
80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9076 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7261 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:
Ayanin
目錄號(hào):
HY-N2913
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