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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。
ML753286图片
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 tmaxvalues 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 tmaxvalues 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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month