Trpm4-in-1 (CBA) is an effective and selective cationic channel TRPM4 inhibitor with an IC50 of 1.5 μM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
|Related TRP Channel Products|
GFB-8438 is a potent subtype selective TRPC5 inhibitor against hTRPC5 and hTRPC4 IC50 0.18 and 0.29 μM, respectively. GFB-8438 has good selectivity for TRPC6, other members of the TRP family, NaV1.5, and limited activity against hERG channels. Protective effect of GFB-8438 on mouse podocytes.
Mavatrep is an orally active TRPV1 antagonist with high affinity for the hTRPV1 channel, inhibits the binding of the TRPV1 agonist to [3H]-Resiniferatoxin (Ki=6.5 nM), and has a low effect on the enzymatic activity of CYP subtypes 3A4, 1A2, and 2D6.
JNJ-17203212 is a selective, highly effective, competitive TRPV1 antagonist. JNJ-17203212 was developed for research on pain management, such as migraines.
Asivatrep (PAC-14028) is a highly selective transient receptor potential vanilla acid subtype 1 (TRPV1) antagonist.
GSK2193874 is a first-in-class orally bioavailable potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist with IC50 values of 2, 5, and 40 nM. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models.
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