CYP3cide - CAS# 1390637-82-7


Catalog No. Size PriceQuantity
M17039-C Contact sales@xcessbio.com for quotation $100

Description

CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism.

Product information

CAS Number: 1390637-82-7

Molecular Weight: 456.59

Formula: C26H32N8

Chemical Name: 1-[(3S)-1-{1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl}pyrrolidin-3-yl]piperidine

Smiles: CC1C=CC(=CC=1)C1=C(C=NN1C)C1=NN(C)C2=NC=NC(=C12)N1C[C@H](CC1)N1CCCCC1

InChiKey: WDWIMDKOXZZYHH-FQEVSTJZSA-N

InChi: InChI=1S/C26H32N8/c1-18-7-9-19(10-8-18)24-21(15-29-31(24)2)23-22-25(32(3)30-23)27-17-28-26(22)34-14-11-20(16-34)33-12-5-4-6-13-33/h7-10,15,17,20H,4-6,11-14,16H2,1-3H3/t20-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

When investigating the inhibitory properties of CYP3cide, an extreme metabolic inactivation efficiency (kinact/KI) of 3300 to 3800 ml • min-1 • μmol-1 is observed using human liver microsomes from donors of nonfunctioning CYP3A5 (CYP3A5 *3/*3). This observed efficiency equated to an apparent KI between 420 and 480 nM with a maximal inactivation rate (kinact) equal to 1.6 min-1. When CYP3cide is tested at a concentration and preincubation time to completely inhibit CYP3A4 in a library of genotyped polymorphic CYP3A5 microsomes, the correlation of the remaining midazolam 1'-hydroxylase activity to CYP3A5 abundance is significant.

Products are for research use only. Not for human use.

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