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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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| 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. |
| Oleoyl Serotonin
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1. |
| ABT-102
ABT-102 (CHEMBL398338) is a potent and highly selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist. |
| MK-2295
MK-2295 (TRPV1 antagonist 5) is a potent TRPV1 antagonist. MK-2295 can be used for the research of chronic pain. |
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