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

CAS: 1390637-82-7 Cat. No.: P408150 分子式: C₂₆H₃₂N₈ 分子量: 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

概要

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

同義語

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]-

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

名前と識別子

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

関連ターゲット（人間）

CYP3A4 Tclin Cytochrome P450 3A4 (4 Activities)

Discover Target: CYP3A4

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

化学的性質と物理的性質

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

よくある質問

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.