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Submit ReviewTadalafil is a potent and highly selective PDE5 inhibitor (IC50 = 5 nM). Exhibits > 2000-fold selectivity for PDE5 over PDEs 1,2,3 and 4 and 1000-fold selectivity over PDE6. Reduces blood pressure in hypertensive rats. Also delays tumor growth in a mouse model via inhibition of MDSC-mediated immunosuppression. Orally bioavailable.
Tadalafil is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 389.4 |
公式 | C22H19N3O4 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 171596-29-5 |
PubChem ID | 110635 |
InChI Key | WOXKDUGGOYFFRN-IIBYNOLFSA-N |
Smiles | [H][C@]12CC3=C([C@@H](C4=CC5=C(C=C4)OCO5)N1C(CN(C2=O)C)=O)NC6=CC=CC=C36 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.94 | 100 |
以下数据基于产品分子量 389.4。 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 | 2.57 mL | 12.84 mL | 25.68 mL |
5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
参考文献是支持产品生物活性的出版物。
Daugan et al (2003) The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues. J.Med.Chem. 46 4533 PMID: 14521415
Serafini et al (2006) Phosphodiesterase-5 inhibition augments endogenous antitumor immunity by reducing myeloid-derived suppressor cell function. J.Exp.Med. 203 2691 PMID: 17101732
If you know of a relevant reference for Tadalafil, please let us know.
关键词: Tadalafil, Tadalafil supplier, phosphodiesterase, 5, PDE5, potent, highly, selective, inhibitors, inhibits, antihypertensive, anticancer, orally, bioavailable, GF196960, Phosphodiesterases, 6311, Tocris Bioscience
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