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
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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]. |
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| Related Catalog | |
| 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 |
| 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 |