883031-03-6
2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
CAS: 883031-03-6
Molecular Formula: C26H28F3N3O2
883031-03-6 - Names and Identifiers
883031-03-6 - Physico-chemical Properties
| Molecular Formula | C26H28F3N3O2 |
| Molar Mass | 471.51 |
| Solubility | DMSO: ≥15mg/mL |
| Appearance | powder |
| Color | white to tan |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| In vitro study | HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells. HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein. HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation. HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis. RT-PCR Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 24 hours Result: The mRNA expression was significantly decreased. Western Blot Analysis Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 24 hours Result: The expression of TRPV4 protein was significantly decreased. Cell Proliferation Assay Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 48 hours Result: Inhibited cell proliferation. Apoptosis Analysis Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 48 hours Result: Promoted cell apoptosis. |
| In vivo study | 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. Animal Model: Cyclophosphamide-treated WT and Trpv4 −/− mice, and naive WT mice Dosage: 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg Administration: Intraperitoneal injection; for 30 minutes Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4 −/− mice. |
883031-03-6 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | R25 - Toxic if swallowed R36 - Irritating to the eyes |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
883031-03-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.119 ml | 10.593 ml | 21.186 ml |
| 5 mM | 0.424 ml | 2.119 ml | 4.237 ml |
| 10 mM | 0.212 ml | 1.059 ml | 2.119 ml |
| 5 mM | 0.042 ml | 0.212 ml | 0.424 ml |
Last Update：2024-01-02 23:10:35
883031-03-6 - Reference Information
| biological activity | HC-067047 is a selective TRPV4 antagonist, the IC50 of rat TRPV4 and mouse TRPV4 were 48 nM,133 nM and 17 nM, respectively. |
| Target | TargetValue mTRPV4 (Cell-free assay) 17 nM hTRPV4 (Cell-free assay) 48 nM rTRPV4 (Cell-free assay) 133 nM |
| Target | Value |
| mTRPV4 (Cell-free assay) | 17 nM |
| hTRPV4 (Cell-free assay) | 48 nM |
| rTRPV4 (Cell-free assay) | 133 nM |
| in vitro study | HC-067047 (1 µm; 24 hours; HEI-OC1 cells) mRNA expression in high glucose cultured HEI-OC1 cells. HC-067047 (1 µm; 24 hours; HEI-OC1 cells) treatment significance claims the expression of TRPV4 protein. HC-067047 (1 µm; 48 hours; HEI-OC1 cells). HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis. RT-PCR Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 24 hours Result: The mRNA expression was significantly decreased. Western Blot Analysis Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 24 hours Result: The expression of TRPV4 protein was significantly decreased. Cell Proliferation Assay Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 48 hours Result: Inhibited cell proliferation. Apoptosis Analysis Cell Line: HEI-OC1 cells Concentration: 1 µM Incubation Time: 48 hours Result: Promoted cell apoptosis. |
| Cell Line: | HEI-OC1 cells HEI-OC1 cells HEI-OC1 cells HEI-OC1 cells |
| Concentration: | 1 µM 1 µM 1 µM 1 µM |
| Incubation Time: | 24 hours 24 hours 48 hours 48 hours |
| Result: | The mRNA expression was significantly decreased. The expression of TRPV4 protein was significantly decreased. Inhibited cell proliferation. Promoted cell apoptosis. Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4 −/− mice. |
| in vivo study | HC-067047 (0-50 mg/kg; Intraperone injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4 −/− mice, and naive WT mice. HC-067047 do not affect blade function in Trpv4 −/− mice. Animal Model: Cyclophosphamide-treated WT and Trpv4 −/− mice, and naive WT mice Dosage: 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg Administration: Intraperitoneal injection; for 30 minutes Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4 −/− mice. |
| Animal Model: | Cyclophosphamide-treated WT and Trpv4 −/− mice, and naive WT mice |
| Dosage: | 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg |
| Administration: | Intraperitoneal injection; for 30 minutes |
Last Update：2024-04-09 21:32:00
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Product Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide Visit Supplier Webpage Request for quotationCAS: 883031-03-6
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Product Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide Visit Supplier Webpage Request for quotationCAS: 883031-03-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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