CP-100356 hydrochloride - CAS:142715-48-8

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CP-100356 hydrochloride

目录号 : KM4071 CAS No. : 142715-48-8 纯度 : 98%

Data Sheet 产品使用指南

CP-100356 hydrochloride 是一种具有口服活性的 MDR1 (P-gp)/BCRP 双重抑制剂，可以抑制 MDR1 介导的 Calcein-AM 转运 (IC₅₀=0.5 µM) 和 BCRP 介导的 Prazosin 转运 (IC₅₀=1.5 µM)。CP-100356 hydrochloride 也是 OATP1B1 的弱抑制剂 (IC₅₀=∼66 µM)。CP-100356 hydrochloride 对 MRP2 和主要的人 P450 酶没有抑制作用 (IC₅₀>15 µM)。

规格	价格	是否有货
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC₅₀s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC₅₀=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC₅₀>15 µM).

体外研究

CP-100356 (0.1-15 µM; pretreated for 30 min) inhibits acetoxymethyl Calcein (Calcein-AM) uptake and and Digoxin transport in human MDR1-transfected MDCKII cells, with IC₅₀s of 0.50 µM and 1.2 µM, respectively. CP-100356 decreases the BCRP-mediated transport of Prazosin in MDCKII cells, with an IC₅₀ of 1.5 µM.
CP-100356 (0.064-200 µM; 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC₅₀ of ~66 µM.
CP-100356 (0-50 µM; 10-30 min) is devoid of inhibition (IC₅₀>50 µM) against the catalytic activity of the individual P450 enzymes including P4503A4 in the competitive inhibition study.

体内研究

CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in C_max and AUC at the dose of 24 mg/kg) in rats.

分子式

C₃₁H₃₆N₄O₆^.HCl

分子量

597.10

CAS号

142715-48-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 44 mg/mL (73.69 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6748 mL	8.3738 mL	16.7476 mL
5 mM	0.3350 mL	1.6748 mL	3.3495 mL
10 mM	0.1675 mL	0.8374 mL	1.6748 mL

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 (sealed storage, away from moisture)。-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。

纯度： 98%