142715-48-8

142715-48-8 structure

Name: CP-100356 hydrochloride
Chemical Name: 4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-N-[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxyquinazolin-2-amine,hydrochloride
CAS Number: 142715-48-8
Molecular Formula: C₃₁H₃₇ClN₄O₆
Molecular Weight: 597.10200
Catalog: Signaling Pathways Membrane Transporter/Ion Channel BCRP
Create Date: 2016-08-12 05:52:18
Modify Date: 2024-01-09 12:40:24
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)[1].

Name	4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-N-[2-(3,4-dimethoxyphenyl)ethyl]-6,7-dimethoxyquinazolin-2-amine,hydrochloride
Synonyms	CP-100356 Hydrochloride

Description	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)[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein Research Areas >> Metabolic Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP
Target	IC50: 0.5 µM (MDR1), 1.5 µM (BCRP) in MDCKII cells[1]
In Vitro	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[1]. CP-100356 (0.064-200 µM; 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC50 of ~66 µM[1]. 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[1].
In Vivo	CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in Cmax and AUC at the dose of 24 mg/kg) in rats[1].
References	[1]. Kalgutkar AS, et, al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J Pharm Sci. 2009 Dec;98(12):4914-27.

Molecular Formula	C₃₁H₃₇ClN₄O₆
Molecular Weight	597.10200
Exact Mass	596.24000
PSA	99.66000
LogP	5.18760

Hazard Codes	Xi
RIDADR	NONH for all modes of transport

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