IMR-1A

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IMR-1A  纯度: 98.23%

IMR-1A 是 IMR-1 的酸代谢物，一种有效的 Notch 抑制剂，IC50 为 0.5 μM。IMR-1A 相对于 IMR-1 的效力增加了 50 倍。IMR-1 在体内可以代谢为 IMR-1A。

IMR-1A

IMR-1A Chemical Structure

CAS No. : 331862-41-0

规格 价格 是否有货 数量
5 mg ￥3000 In-stock
10 mg ￥4500 In-stock
50 mg ￥12000 In-stock
100 mg ￥17000 In-stock
200 mg   询价  
500 mg   询价  

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IMR-1A 相关产品

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生物活性

IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A[1].

IC50 & Target

IC50: 0.5 μM (Notch)[1]
体内研究
(In Vivo)

IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57 BL/6 mice[1]
Dosage: 2 mg/kg (i.v.) and 100 mg/kg (i.p)
Administration: I.v. and i.p.
Result: Exhibited low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration and plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.

分子量

325.36

Formula

C13H11NO5S2
CAS 号

331862-41-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 2 mg/mL (6.15 mM; Need ultrasonic)

H2O : 1 mg/mL (3.07 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0735 mL 15.3676 mL 30.7352 mL
5 mM 0.6147 mL 3.0735 mL 6.1470 mL
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.

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