GSK 2193874

• Supplier: Tocris Bioscience
• Catalog: 5694
• Prices: $209.00, $879.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 1336960-13-4
• Chemical Name: 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
• Formula: C37H38BrF3N4O
• Molecular Weight: 691.62
• Description: Potent and selective TRPV4 antagonist (IC 50 values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca 2+ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.

Product References

An orally active TRPV4 channel blocker prevents and resolves pulmonary edema - An orally active TRPV4 channel blocker prevents and resolves pulmonary edema

Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN. Sci Transl Med. 2012 Nov 7;4(159):159ra148.