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PFI 653

Cat. No. 7963 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective vanin 1 inhibitor
化学名： 8-Oxa-2-azaspiro[4.5]dec-2-yl[2-[(2-pyrazinylmethyl)amino]-5-pyrimidinyl]methanone
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for PFI 653

PFI 653 is a potent and selective vanin 1 inhibitor (IC50 values in the range 6.85 - 24.5 nM). The compound exhibits selectivity over a panel of 40 kinases and a selection of 35 other targets including enzymes, receptors and ion channels (IC50 vs biotinidase > 50 μM). Following administration of a single dose of PFI 653 (2 mg/kg iv) in rats AUC is 1790 ng.h/mL, half-life is 1 h and clearance is 19 mL/min/kg. Following oral administration of PFI 653 in solution, bioavailablility is 96%. In mice with DSS-induced inflammatory bowel disease (IBD), oral adminstration of PFI 653 dose-dependently reduces vanin 1 enzyme activity and disease symptoms.

许可信息

This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the PFI-653 probe summary on the SGC website.

技术数据 for PFI 653

分子量 354.41
公式 C18H22N6O2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2173134-00-2
PubChem ID 134177597
InChI Key VGRLXWFIXGZRMS-UHFFFAOYSA-N
Smiles O=C(C1=CN=C(N=C1)NCC2=NC=CN=C2)N3CCC4(C3)CCOCC4

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PFI 653

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 1.77 5
DMSO 35.44 100

制备储备液 for PFI 653

以下数据基于产品分子量 354.41。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.82 mL 14.11 mL 28.22 mL
5 mM 0.56 mL 2.82 mL 5.64 mL
10 mM 0.28 mL 1.41 mL 2.82 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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参考文献 for PFI 653

参考文献是支持产品生物活性的出版物。

Casimiro-Garcia et al (2022) Discovery of a series of pyrimidine carboxamides as inhibitors of vanin-1. J.Med.Chem. 65 757 PMID: 34967602

If you know of a relevant reference for PFI 653, please let us know.

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关键词: PFI 653, PFI 653 supplier, PFI653, vanin, 1, potent, selective, inhibitor, inhibits, inflammatory, bowel, disease, IBD, Other, Hydrolases, 7963, Tocris Bioscience

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