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.
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
Molecular Weight | 471.51 |
Formula | C26H28F3N3O2 |
CAS Number | 883031-03-6 |
Purity | 99.64% |
Solubility | DMSO: ≥15 mg/mL |
Storage | at -20°C |
[2] Fumio Nakagawa, et al. Modification of TRPV4 activity by acetaminophen
Related TRP Channel Products |
---|
TRPM4-IN-1
Trpm4-in-1 (CBA) is an effective and selective cationic channel TRPM4 inhibitor with an IC50 of 1.5 μM. |
GFB-8438
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
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
JNJ-17203212 is a selective, highly effective, competitive TRPV1 antagonist. JNJ-17203212 was developed for research on pain management, such as migraines. |
Asivatrep
Asivatrep (PAC-14028) is a highly selective transient receptor potential vanilla acid subtype 1 (TRPV1) antagonist. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.