Cav 3.2 inhibitor 2 是Cav3.2 T-type Ca2+channels的抑制剂,在 -80mV 恒定电位下的IC50值为 0.09339 μM。Cav 3.2 inhibitor 2 能有效抑制小鼠 T 通道依赖性的躯体和内脏疼痛。Cav 3.2 inhibitor 2 可用于顽固性疼痛的研究。
产品描述
Cav 3.2 inhibitor 2 is a Ca v 3.2 T-type Ca 2+ channels inhibitor with an IC 50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain [1].
体外活性
Cav 3.2 inhibitor 2 (0.3 μM) shows a produced inhibition of Ca v 3.2 comparable to that of pimozide [1]. Cav 3.2 inhibitor 2 (1 and 10 μM; 90 min) shows a binding affinity to D2 receptor significantly less than pimozide [1]. Cav 3.2 inhibitor 2 (0.01-10 μM) inhibits T channels isoforms with IC 50 s of 0.09339, 1.109 and 0.2167 μM for -80mV Ca v 3.2, -110mV Ca v 3.2 and Ca v 3.1, respectively [1].
体内活性
Cav 3.2 inhibitor 2 (1-10 mg/kg; i.p. 30 min before i.pl. Na 2 S) affects the Na 2 S-induced pain in vivo [1]. Cav 3.2 inhibitor 2 (10 mg/kg; i.p. 7 days after oxaliplatin treatment) affects oxaliplatin-induced allodynia in vivo [1]. Animal Model: Mice with Na 2 S intraplantar (i.pl.) administration [1] Dosage: 1, 3 and 10 mg/kg Administration: Intraperitoneal injection; 1-10 mg/kg 30 min before i.pl. Na 2 S Result: Almost completely blocked the Na 2 S-induced colonic pain and referred hyperalgesia. Animal Model: Wild-type (WT) or Ca v 3.2-kockout (KO) C57BL/6 mice with oxaliplatin (OHP) injection [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg on day 7 after oxaliplatin treatment Result: Attenuated the oxaliplatin-induced allodynia in WT C57BL/6 mice, while showed no effect on KO mice.
分子式
C32H37F2N3O
分子量
517.65
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years