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Submit ReviewPF 915275
说明： Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor
化学名： N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide
纯度： ≥98% (HPLC)
生物活性 for PF 915275
PF 915275 is a potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) that displays little activity at 11βHSD2 (1.5% inhibition at 10 μM). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC50 = 15 nM) and has antidiabetic activity in vivo. Orally active.
化合物库 for PF 915275
PF 915275 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for PF 915275
| 分子量 | 350.39 |
| 公式 | C18H14N4O2S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 857290-04-1 |
| PubChem ID | 23725123 |
| InChI Key | ZESFDAKNYJQYKO-UHFFFAOYSA-N |
| Smiles | NC1=NC(NS(C(C=C3)=CC=C3C2=CC=C(C#N)C=C2)(=O)=O)=CC=C1 |
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 PF 915275
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.04 | 100 |
制备储备液 for PF 915275
以下数据基于产品分子量 350.39。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.85 mL | 14.27 mL | 28.54 mL |
| 5 mM | 0.57 mL | 2.85 mL | 5.71 mL |
| 10 mM | 0.29 mL | 1.43 mL | 2.85 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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产品说明书 for PF 915275
参考文献 for PF 915275
参考文献是支持产品生物活性的出版物。
Bhat et al (2008) Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monke J.Pharmacol.Exp.Ther. 324 299 PMID: 17921190
Fotsch and Wang (2008) Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 51 4851 PMID: 18652443
Courtney et al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550 PMID: 17986636
If you know of a relevant reference for PF 915275, please let us know.
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关键词: PF 915275, PF 915275 supplier, Potent, selective, 11β-hydroxysteroid, beta-hydroxysteroid, dehydrogenases, type, 1, 11βHSD1, 11betaHSD1, inhibitors, inhibits, PF915275, 11b-Hydroxysteroid, Dehydrogenase, 3291, Tocris Bioscience
3 篇 PF 915275 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 915275 的部分引用包括：
Matsumura et al (2018) Local cortisol activation is involved in EGF-induced immunosuppression. Dermatoendocrinol 9 e1412018 PMID: 29484105
Youm et al (2013) Local blockade of glucocorticoid activation reverses stress- and glucocorticoid-induced delays in cutaneous wound healing. Wound Repair Regen 21 715 PMID: 23927023
Chang (2018) An inhibitor of 11-β hydroxysteroid dehydrogenase type 1 (PF915275) alleviates nonylphenol-induced hyperadrenalism and adiposity in rat and human cells. BMC Pharmacol Toxicol 19 45 PMID: 30021644
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