BCTC

SKU: orb1225121

Description

A highly potent, selective, CNS-penetrant TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively; shows selectivity against 63 other receptor, enzyme, transporter, and ion channel targets; orally bioavailable.Pain Preclinical.

Key Properties

• CAS Number: 393514-24-4
• MW: 372.8917
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₅ClN₄O
• SMILES: O=C(N1CCN(C2=NC=CC=C2Cl)CC1)NC3=CC=C(C(C)(C)C)C=C3
• Target: TRP/TRPV Channel
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: Capsaicin-induced Sprague-Dawley rats model. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg. Administration: Oral gavage (p.o.), Single dose. Before capsaicin (HY-10448) treatment (30 μg; intraplantar injection; Single dose). Result: Inhibited capsaicin-mediated thermal hyperalgesia in a dose-dependent manner. Animal model: Freund’s complete adjuvant (FCA) Sprague-Dawley rats model. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg. Administration: Oral gavage (p.o.), Single dose. After 100 % FAC treatment (50 μL; intraplantar injection; Single dose). Result: Significantly reduced FAC-induced inflammation-related thermal pain and mechanical hyperalgesia, and extended the inhibitory effect of mechanical hyperalgesia to 6 h at high doses (10 mg/kg, 30 mg/kg). Animal model: Partial sciatic nerve ligation Sprague-Dawley rats model. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg. Administration: Oral gavage (p.o.), Single dose. After partial sciatic nerve ligation. Result: Reduced post-operative abnormal tactile pain and mechanical hyperalgesia in a dose-dependent manner. Animal model: Particularly strong insulin resistance and hyperinsulinemia ob/ob mice model. Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg. Administration: Oral gavage (p.o.); Twice daily for 4 weeks. Result: Reduced plasma triglyceride and glucose area under the curve (AUC) level.
• In Vitro:
  Western blot analysis. Cell line: DU145. Concentration: 20 μM, 40 μM, 60 μM, 80 μM, 100 μM. Incubation time: 48 h. Result: Down-regulated p-Akt, while p-GSK-3β was up-regulated leaving their unphosphorylated form unchanged. Significantly down-regulated Cyclin D1(20), the most relevant protein in the cell cycle, without affecting cyclin-B1.Reduced the expression of CDK2 and CDK6, but without affecting the expression level of CDK4.Downregulates MMP2 and p-FAK levels. Cell Viability Assay Cell line: DU145, PNT1A. Concentration: 20 μM, 40 μM, 60 μM, 80 μM, 100 μM. Incubation time: 72 h. Result: Decreased the growth of DU145 cells in a concentration-dependent manner, with 12.03% and 50.69% growth inhibition at 10 μM and 100 μM, respectively, but had little effect on normal prostate PNT1A cells.

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

BCTC

Quick Database Links

Gene Symbol

TRP/TRPV Channel