BCTC

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性、中枢神经系统渗透性 TRPV1 拮抗剂，可抑制辣椒素诱导和酸诱导的大鼠 TRPV1 激活，IC50 值分别为 35 和 6 nM。

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.

Western Blot AnalysisCell Line:DU145Concentration:20 μM, 40 μM, 60 μM, 80 μM,100 μM Incubation Time:48 hResult: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.

Animal Model:Capsaicin-induced Sprague-Dawley rats modelDosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kgAdministration: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 modelDosage: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.

BCTC

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Pain

393514-24-4

372.8917

C20H25ClN4O

>98% (HPLC)

10 mM in DMSO

O=C(N1CCN(C2=NC=CC=C2Cl)CC1)NC3=CC=C(C(C)(C)C)C=C3

1-Piperazinecarboxamide, 4-(3-chloro-2-pyridinyl)-N-[4-(1,1-dimethylethyl)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years