BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
| Molecular Weight | 442.43 |
| CAS Number | 2361241-23-6 |
| Solubility (25°C) | DMSO 31.25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[3] Zhihuang Zheng, et al. Role of TRPC6 in kidney damage after acute ischemic kidney injury
[4] Pritesh P Jain, et al. TRPC6, a therapeutic target for pulmonary hypertension
| Related TRP Channel Products |
|---|
| N-Oleoyl glutamine
N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). |
| N-Oleoyl valine
N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist. |
| TAT-M2NX
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. |
| SOR-C13
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. |
| GsMTx4 TFA
GsMTx4 TFA is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. In addition, GsMTx4 TFA blocks cation-selective stretch-activated channels (SACs) and attenuates lysophosphatidylcholine (LPC)-induced astrocytotoxicity and microglial cell reactivity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
