HC-067047

SKU: orb1221687

Description

HC-067047 is a potent and selective TRPV4 antagonist. HC-067047 increases functional bladder capacity and reduces micturition frequency in WT mice and rats with cystitis. HC-067047 did not affect bladder function in Trpv4(-/-) mice, demonstrating that its in vivo effects are on target. HC-067047 may provide a promising means of treating bladder

Key Properties

• CAS Number: 883031-03-6
• MW: 471.51
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₈F₃N₃O₂
• SMILES: FC(F)(F)c1cc(ccc1)NC(=O)c4cc(c2ccccc2)n(CCCN3CCOCC3)c4C
• Target: hTRPV4/mTRPV4
• Solubility: DMSO : 50 mg/mL 106.04 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HC-067047 | HC 067047 | HC067047

Quick Database Links

Gene Symbol

hTRPV4/mTRPV4