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MedKoo CAT#: 526697
CAS#: 866206-54-4
Description: 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]).
MedKoo Cat#: 526697
Name: PRX-08066 free base
CAS#: 866206-54-4
Chemical Formula: C19H17ClFN5S
Exact Mass: 401.0877
Molecular Weight: 401.8884
Elemental Analysis: C, 56.78; H, 4.26; Cl, 8.82; F, 4.73; N, 17.43; S, 7.98
Related CAS #: 866206-55-5(PRX-08066 Maleate)
Synonym: PRX-08066; PRX 08066; PRX08066.
IUPAC/Chemical Name: 5-((4-(6-Chlorothieno(2,3-d)pyrimidine-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile
InChi Key: RPYIKXHIQXRXEM-BTJKTKAUSA-N
InChi Code: InChI=1S/C19H17ClFN5S.C4H4O4/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;5-3(6)1-2-4(7)8/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25);1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code: N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F
1: Kim SK, Li Y, Abrol R, Heo J, Goddard WA 3rd. Predicted structures and
dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C
receptors. J Chem Inf Model. 2011 Feb 28;51(2):420-33. doi: 10.1021/ci100375b.
Epub 2011 Feb 7. PubMed PMID: 21299232; PubMed Central PMCID: PMC3070210.
2: Svejda B, Kidd M, Giovinazzo F, Eltawil K, Gustafsson BI, Pfragner R, Modlin
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10.1002/cncr.25049. PubMed PMID: 20564397.
3: Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ,
Shacham S, Al-Mousily F. PRX-08066, a novel 5-hydroxytryptamine receptor 2B
antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and
right ventricular hypertrophy in rats. J Pharmacol Exp Ther. 2010
Aug;334(2):364-72. doi: 10.1124/jpet.109.165001. Epub 2010 Apr 29. PubMed PMID:
20430844.
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