IMR-1A

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IMR-1A

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

331862-41-0

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。

生物活性

IMR-1A, a acid metabolite of IMR-1, is aNotchinhibitor with anIC₅₀of 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].

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

性状

Solid

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℃)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。