HC 067047
HC067047 is a selective TRPV4 antagonist with IC50 of 48 nM, 133 nM and 17 nM for human, rat and mouse TRPV4, respectively[1].
In HEI-OC1 cells, HC067047 (1 µM) treatment for 24 hours can significantly reduce the mRNA expression in HEI-OC1 cells cultured in high glucose and reduce the expression of TRPV4 protein. HC067047 (1 µM) treatment for 48 hours can inhibit cell proliferation and promote apoptosis[2].
In WT mice with cystiti, HC067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes) treatment increases functional bladder capacity and reduces micturition frequency. HC067047 do not affect bladder function in Trpv4−/− mice[1].
References:
[1]. Everaerts W et al. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.Proc Natl Acad Sci U S A, 2010, 107(44): 19084-9.
[2]. Xing Y, et al. Decreased Expression of TRPV4 Channels in HEI-OC1 Cells Induced by High Glucose Is Associated with Hearing Impairment. Yonsei Med J, 2018, 59(9): 1131-1137.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 471.51 |
| Cas No. | 883031-03-6 |
| Formula | C26H28F3N3O2 |
| Solubility | ≥47.2 mg/mL in DMSO; insoluble in H2O; ≥16.83 mg/mL in EtOH with ultrasonic |
| Chemical Name | 2-methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(C1=CC(NC(C2=C(C)N(C(C3=CC=CC=C3)=C2)CCCN4CCOCC4)=O)=CC=C1)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
