HC 067047 |
| Catalog No.GC12260 |
HC 067047 est un antagoniste puissant et sélectif de TRPV4 et inhibe de manière réversible les courants à travers les orthologues de TRPV4 humain, rat et souris avec des valeurs IC50 de 48 nM, 133 nM et 17 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 883031-03-6
Sample solution is provided at 25 µL, 10mM.
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively[1].
HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells[2].HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis[2].
HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4−/− mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 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 Nov 2;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 Nov;59(9):1131-1137.
| Cas No. | 883031-03-6 | SDF | |
| Chemical Name | 2-methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide | ||
| Canonical SMILES | FC(F)(C1=CC(NC(C2=C(C)N(C(C3=CC=CC=C3)=C2)CCCN4CCOCC4)=O)=CC=C1)F | ||
| Formula | C26H28F3N3O2 | M.Wt | 471.51 |
| Solubility | ≥ 47.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1208 mL | 10.6042 mL | 21.2085 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2417 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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