HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively.
|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: ≥15 mg/mL|
|Related TRP Channel Products|
Trpm4-in-1 (CBA) is an effective and selective cationic channel TRPM4 inhibitor with an IC50 of 1.5 μM.
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.
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