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GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist with IC50 values of 2, 5, and 40 nM. It is selective for TRPV4 over ~200 other human receptors, channels, and enzymes. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models. GSK2193874 shows low clearance (7.3 mL/min/kg) and good rat oral bioavailability (31%).
| Molecular Weight | 691.62 |
| Formula | C37H38BrF3N4O |
| CAS Number | 1336960-13-4 |
| Solubility (25°C) | DMSO ≥ 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related TRP Channel Products |
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| PF-04745637
PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1. |
| Phenazopyridine
Phenazopyridine is a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine is a TRPM8 antagonist. Phenazopyridine can promote neuronal differentiation and it can also be used in the research of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases. |
| 4-ONE
4-ONE is one of the major hemolytic decomposition products of lipid hydroperoxides. 4-ONE is a potent transient receptor potential ankyrin 1 (TRPA1) agonist. |
| Moringin
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. |
| (S)-ABT-102
(S)-ABT-102 is a potent TRPV1 antagonist, with an IC50 of 123 nM. (S)-ABT-102 can block the activation of TRPV1 by capsaicin. |
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