Potent (IC 50 = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5. It displayed excellent selectivity against other TRP family members as well as NaV1.5, 50 kinases and 87 other receptor targets along with good pharmacokinetic properties. GFB-8438 protected mouse...
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Potent (IC 50 = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5. It displayed excellent selectivity against other TRP family members as well as NaV1.5, 50 kinases and 87 other receptor targets along with good pharmacokinetic properties. GFB-8438 protected mouse podocytes from injury induced by protamine sulfate and demonstrated efficacy in a hypertensive DOCA-salt rat model suggesting potential therapeutic use for the treatment of chronic kidney disease
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