产品
编 号：F346135
分子式：C20H25ClN4O
分子量：372.89
分子式：C20H25ClN4O
分子量：372.89
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
480
In-stock
10mg
640
In-stock
50mg
2240
In-stock
结构图
CAS No: 393514-24-4
产品详情
生物活性：
BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects.
体内研究：
BCTC (1-30 mg/kg; 口服给药; 单剂量) 可以通过靶向 VR1 来抑制 Sprague-Dawley 大鼠的炎症性和神经性的热痛觉和机械性痛觉过敏，具有镇痛作用。BCTC (10-100 mg/kg; 口服给药，一天2次连续4周) 可以改善糖尿病 ob/ob 小鼠的胰岛素抵抗和全身糖脂代谢，增加胰岛素的分泌。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.Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.
体外研究：
BCTC (20-100 μM; 72 h) 对 DU145 细胞有高选择性的抗肿瘤活性。BCTC (20-100 μM; 48 h) 通过选择性的调节细胞周期调节蛋白亚群的表达水平来诱导细胞周期阻滞在G0/G1 期，且不引发细胞凋亡。BCTC (10 μM 和 100 μM; 48 h) 抑制细胞的迁移和侵袭。BCTC (3-300 nM) 可以通过抑制辣椒素 (300 nM) 诱导的大鼠脊髓切片中降钙素基因相关肽样免疫反应性 (CGRP-LI) (IC50=37.0 nM) 和 p 样物质免疫反应性 (SP-LI) (IC50=36.0 nM) 的释放，从而有效抑制大鼠脊髓 TRPV1 功能。
BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects.
体内研究：
BCTC (1-30 mg/kg; 口服给药; 单剂量) 可以通过靶向 VR1 来抑制 Sprague-Dawley 大鼠的炎症性和神经性的热痛觉和机械性痛觉过敏，具有镇痛作用。BCTC (10-100 mg/kg; 口服给药，一天2次连续4周) 可以改善糖尿病 ob/ob 小鼠的胰岛素抵抗和全身糖脂代谢，增加胰岛素的分泌。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.Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.
体外研究：
BCTC (20-100 μM; 72 h) 对 DU145 细胞有高选择性的抗肿瘤活性。BCTC (20-100 μM; 48 h) 通过选择性的调节细胞周期调节蛋白亚群的表达水平来诱导细胞周期阻滞在G0/G1 期，且不引发细胞凋亡。BCTC (10 μM 和 100 μM; 48 h) 抑制细胞的迁移和侵袭。BCTC (3-300 nM) 可以通过抑制辣椒素 (300 nM) 诱导的大鼠脊髓切片中降钙素基因相关肽样免疫反应性 (CGRP-LI) (IC50=37.0 nM) 和 p 样物质免疫反应性 (SP-LI) (IC50=36.0 nM) 的释放，从而有效抑制大鼠脊髓 TRPV1 功能。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备