AS1842856

AS1842856 是一種特異性的 Foxo1 抑制劑，IC50 為 30 nM，AS1842856 有效抑制自噬 (autophagy)。AS1842856 僅通過與 FoxO1 結(jié)合而降低 FoxO1 的活性，而不影響其轉(zhuǎn)錄和蛋白質(zhì)表達。貨號：HY-100596 ，CAS：836620-48-5

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-100596

起訂量：1

規(guī)格:：5mg

價格:：￥850

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產(chǎn)品詳情

AS1842856

AS1842856 是一種特異性的 Foxo1 抑制劑，IC₅₀ 為 30 nM，AS1842856 有效抑制自噬 (autophagy)。AS1842856 僅通過與 FoxO1 結(jié)合而降低 FoxO1 的活性，而不影響其轉(zhuǎn)錄和蛋白質(zhì)表達。

生物活性

AS1842856, a specific Foxo1 inhibitor (IC₅₀=30 nM), potently suppresses autophagy^[1]. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression

IC₅₀ & Target

IC50: 30 nM (Foxo1)

體外研究(In Vitro)

AS1842856 potently inhibits human Foxo1 transactivation and reduces glucose production through the inhibition of glucose-6 phosphatase and phosphoenolpyruvate carboxykinase mRNA levels in a rat hepatic cell line^[1]. After AS1842856 treatment, there is no significant difference in the protein expression of p-FoxO1 and FoxO1 compared with the control group, but the expression of p-Akt is decreased compared with the control group

體內(nèi)研究(In Vivo)

Oral administration of AS1842856 to diabetic db/db mice leads to a drastic decrease in fasting plasma glucose level via the inhibition of hepatic gluconeogenic genes, whereas administration to normal mice has no effect on the fasting plasma glucose level. Treatment with AS1842856 also suppresses an increase in plasma glucose level caused by pyruvate injection in both normal and db/db mice

分子量:347.38

Formula:C₁₈H₂₂FN₃O₃

CAS 號:836620-48-5

運輸條件:Room temperature in continental US; may vary elsewhere.

儲存方式:

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

DMSO : 5 mg/mL (14.39 mM; ultrasonic and warming and heat to 60°C)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.8787 mL	14.3935 mL	28.7869 mL
5 mM	0.5757 mL	2.8787 mL	5.7574 mL
10 mM	0.2879 mL	1.4393 mL	2.8787 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；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

1.

請依序添加每種溶劑： 6% HP-β-CD in saline
Solubility: 10 mg/mL (28.79 mM); Suspension solution; Need ultrasonic
2.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (4.81 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1 mg/mL (2.88 mM); Suspended solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.88 mM); Clear solution

參考文獻

[1]. Nagashima T, et al. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol Pharmacol. 2010 Nov;78(5):961-70.

[2]. He J, et al. The resistant effect of SIRT1 in oxidative stress-induced senescence of rat nucleus pulposus cell is regulated by Akt-FoxO1 pathway. Biosci Rep. 2019 May 10;39(5). pii: BSR20190112.

AS1842856

AS1842856 是一種特異性的 Foxo1 抑制劑，IC50 為 30 nM，AS1842856 有效抑制自噬 (autophagy)。AS1842856 僅通過與 FoxO1 結(jié)合而降低 FoxO1 的活性，而不影響其轉(zhuǎn)錄和蛋白質(zhì)表達。貨號：HY-100596 ，CAS：836620-48-5

品牌：MCE

型號：HY-100596

起訂量：1

規(guī)格:：5mg

價格:：￥850

15906629305

在線客服

客服一

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產(chǎn)品詳情

AS1842856

AS1842856 是一種特異性的 Foxo1 抑制劑，IC₅₀ 為 30 nM，AS1842856 有效抑制自噬 (autophagy)。AS1842856 僅通過與 FoxO1 結(jié)合而降低 FoxO1 的活性，而不影響其轉(zhuǎn)錄和蛋白質(zhì)表達。

生物活性

AS1842856, a specific Foxo1 inhibitor (IC₅₀=30 nM), potently suppresses autophagy^[1]. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression

IC₅₀ & Target

IC50: 30 nM (Foxo1)

體外研究(In Vitro)

AS1842856 potently inhibits human Foxo1 transactivation and reduces glucose production through the inhibition of glucose-6 phosphatase and phosphoenolpyruvate carboxykinase mRNA levels in a rat hepatic cell line^[1]. After AS1842856 treatment, there is no significant difference in the protein expression of p-FoxO1 and FoxO1 compared with the control group, but the expression of p-Akt is decreased compared with the control group

體內(nèi)研究(In Vivo)

Oral administration of AS1842856 to diabetic db/db mice leads to a drastic decrease in fasting plasma glucose level via the inhibition of hepatic gluconeogenic genes, whereas administration to normal mice has no effect on the fasting plasma glucose level. Treatment with AS1842856 also suppresses an increase in plasma glucose level caused by pyruvate injection in both normal and db/db mice

分子量:347.38

Formula:C₁₈H₂₂FN₃O₃

CAS 號:836620-48-5

運輸條件:Room temperature in continental US; may vary elsewhere.

儲存方式:

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

DMSO : 5 mg/mL (14.39 mM; ultrasonic and warming and heat to 60°C)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.8787 mL	14.3935 mL	28.7869 mL
5 mM	0.5757 mL	2.8787 mL	5.7574 mL
10 mM	0.2879 mL	1.4393 mL	2.8787 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；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

1.

請依序添加每種溶劑： 6% HP-β-CD in saline
Solubility: 10 mg/mL (28.79 mM); Suspension solution; Need ultrasonic
2.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (4.81 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1 mg/mL (2.88 mM); Suspended solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.88 mM); Clear solution

參考文獻

[1]. Nagashima T, et al. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol Pharmacol. 2010 Nov;78(5):961-70.

[2]. He J, et al. The resistant effect of SIRT1 in oxidative stress-induced senescence of rat nucleus pulposus cell is regulated by Akt-FoxO1 pathway. Biosci Rep. 2019 May 10;39(5). pii: BSR20190112.

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AS1842856

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AS1842856