PF-4981517 - 10mM in DMSO , CAS No.1390637-82-7

CAS: 1390637-82-7 Cat. No.: P408150 Formule: C₂₆H₃₂N₈ Poids moléculaire: 456.59

GRADE & PURITY 10mM in DMSO

Synonyms

CYP3cide, PF-04981517 | 1H-Pyrazolo[3,4-d]pyrimidine, 1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-(1-piperidinyl)-1-pyrrolidinyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

Information

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor ofCYP3A4(P450) withIC50of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
In vitro

PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. PF-4981517 is tested as a reversible inhibitor of several human cytochrome P450 activities in pooled HLMs. PF-4981517 is selective for CYP3A4 with IC50 of 0.03 μM, 17 μM and 70 μM for CYP3A4, 3A5, and 3A7, respectively. PF-4981517 is a mechanism-based inactivator. PF-4981517 serves as an important in vitro tool, which when used side-by-side with ketoconazole to inhibit all CYP3A activity will permit distinction between the contribution of CYP3A4 to CYP3A5 (as well as CYP3A7 and maybe CYP3A43). PF-4981517 is useful to investigators seeking to delineate the relative contribution of CYP3A4 versus CYP3A5 in the metabolism of compounds cleared by CYP3A.

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonymes

CYP3cide, PF-04981517 | 1H-Pyrazolo[3,4-d]pyrimidine, 1-methyl-3-[1-methyl-5-(4-methylphenyl)-1H-pyrazol-4-yl]-4-[(3S)-3-(1-piperidinyl)-1-pyrrolidinyl]-

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Noms et identifiants

• Isomères SMILES: CC1=CC=C(C=C1)C2=C(C=NN2C)C3=NN(C4=C3C(=NC=N4)N5CC[C@@H](C5)N6CCCCC6)C
• Poids moléculaire: 456.59
• Reaxy-Rn: 29238478
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29238478&ln=

Cibles associées (humaines)

CYP3A4 Tclin Cytochrome P450 3A4 (4 Activities)

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriétés chimiques et physiques

• Solubilité: Solubility (25°C) In vitro DMSO: 56 mg/mL (197.0 mM)

Foire aux questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1390637-82-7, the molecular formula is C26H32N8, and the molecular weight is 456.59 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.