英文名称 | praliciguat |
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别名 | IW-1973;IW1973 |
英文别名 | IW-1973;IW1973 |
IUPAC Name | 1,1,1,3,3,3-hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)pyrazol-3-yl]pyrimidin-4-yl]amino]methyl]propan-2-ol |
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INCHI | InChI=1S/C21H14F8N6O2/c22-12-4-2-1-3-11(12)9-35-16(14-5-6-37-34-14)7-15(33-35)18-30-8-13(23)17(32-18)31-10-19(36,20(24,25)26)21(27,28)29/h1-8,36H,9-10H2,(H,30,31,32) |
InChi Key | CYSJNTQNMDWAJV-UHFFFAOYSA-N |
Canonical SMILES | C1=CC=C(C(=C1)CN2C(=CC(=N2)C3=NC=C(C(=N3)NCC(C(F)(F)F)(C(F)(F)F)O)F)C4=NOC=C4)F |
关联CAS | 1628730-49-3 |
PubChem CID | 86269973 |
MeSH Entry Terms | 1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazol-3-yl) pyrimidin-4-yl)amino)methyl)propan-2-ol;IW-1973;praliciguat |
CAS Registry No. | 1628730-49-3 |
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PubChem CID | 86269973 |
Ligand ID | 9900 |
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名称 | praliciguat |
别名 | IW-1973 |
类别 | Synthetic organic |
学名 | 1,1,1-trifluoro-3-[(5-fluoro-2-{1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)-1H-pyrazol-3-yl}pyrimidin-4-yl)amino]-2-(trifluoromethyl)propan-2-ol |
生物活性评价 |
Praliciguat (IW-1973)-induced prevention of inflammation and fibrosis in experimental non-alcoholic steatohepatitis was reported in early 2018 |
评价 |
Praliciguat (IW-1973) is a potent, orally available soluble guanylyl cyclase (sGC) stimulator |
临床描述 |
The objective of the CAPACITY-HFpEF study is to evaluate the safety and efficacy of IW-1973 compared with placebo when administered daily for approximately 12 weeks to patients with HFpEF. The study will evaluate the effect of oral IW-1973 on peak exercise capacity in patients with HFpEF, with or without permanent or persistent atrial fibrillation. |
来源公司 |
Cyclerion Therapeutics |
1. Breitenstein S, Roessig L, Sandner P, Lewis KS. (2017) Novel sGC Stimulators and sGC Activators for the Treatment of Heart Failure.. Handb Exp Pharmacol, 243 (13): (225-247). [PMID:27900610] |
2. Flores-Costa R, Alcaraz-Quiles J, Titos E, López-Vicario C, Casulleras M, Duran-Güell M, Rius B, Diaz A, Hall K, Shea C et al.. (2018) The soluble guanylate cyclase stimulator IW-1973 prevents inflammation and fibrosis in experimental non-alcoholic steatohepatitis.. Br J Pharmacol, 175 (6): (953-967). [PMID:29281143] |
3. Tobin JV, Zimmer DP, Shea C, Germano P, Bernier SG, Liu G, Long K, Miyashiro J, Ranganath S, Jacobson S et al.. (2018) Pharmacological Characterization of IW-1973, a Novel Soluble Guanylate Cyclase Stimulator with Extensive Tissue Distribution, Antihypertensive, Anti-Inflammatory, and Antifibrotic Effects in Preclinical Models of Disease.. J Pharmacol Exp Ther, 365 (3): (664-675). [PMID:29643251] |