PRX-08066 is a a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. In the 5-HT(2B) expressing SI-NET cell line, KRJ-I, PRX-08066 inhibited proliferation (IC(50) 4.6 x 10(-9)M) and 5-HT secretion (6.9 x 10(-9)M) and decreased ERK1/2 phosphorylation and profibrotic growth factor synthesis and secretion (transforming growth factor beta 1 [TGFbeta1], connective tissue growth factor [CTGF] and fibroblast growth factor [FGF2]).
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化学信息
名称 | PRX-08066 |
Iupac 化学名称 | 5-((4-(6-Chlorothieno(2,3-d)pyrimidine-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile |
同义词 | PRX-08066; PRX 08066 |
英文同义词 | PRX-08066; PRX 08066 |
分子式 | C19H17ClFN5S |
分子量 | 401.8884 |
Smile | ClC1=CC2=C(N=CN=C2NC2CCN(CC2)CC=2C=CC(=C(C#N)C2)F)S1 |
InChiKey | IENZFHBNCRQMNP-UHFFFAOYSA-N |
InChi | InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25) |
Cas号 | 866206-54-4 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |