ML753286

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ML753286

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:

1699720-89-2

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

ML753286 是一种口服活性和选择性BCRP(抗乳腺癌蛋白) 抑制剂，IC₅₀为 0.6 μM。 ML753286 在啮齿动物和人类肝脏 S9 组分中具有高渗透性和低至中等清除率，并且在不同物种中都具有血浆稳定性。

生物活性

ML753286 is an orally active and selectiveBCRP(Breastcancerresistance protein)inhibitor with anIC₅₀of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species^[1].

IC₅₀& Target

IC50: 0.6 μM (BCRP)^[1]

体外研究
(In Vitro)

ML753286 has IC₅₀values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively^[1].

体内研究
(In Vivo)

ML753286 (25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV); 0.083-24 hours) appears to completely inhibit Bcrp functions in rats at 25 mg/kg PO or at 20 mg/kg IV. The t_maxvalues in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively^[1].

Animal Model:	Male Bcrp KO (Abcg2–/–) and WT (Wistar) Rats^[1]
Dosage:	25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV) (Pharmacokinetic Study)
Administration:	PO or IV; 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours
Result:	The t_maxvalues in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively.

分子量

355.43

性状

Solid

Formula

C₂₀H₂₅N₃O₃

CAS 号

1699720-89-2

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