| Bioactivity | Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca2+ channels inhibitor with an IC50 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]. |
| Target | IC50: 0.09339 μM (-80mV Cav3.2), 1.109 μM (-110mV Cav3.2), 0.2167 μM (Cav3.1) |
| Invitro | Cav 3.2 inhibitor 2 (0.3 μM) shows a produced inhibition of Cav3.2 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 IC50s of 0.09339, 1.109 and 0.2167 μM for -80mV Cav3.2, -110mV Cav3.2 and Cav3.1, respectively[1]. |
| In Vivo | Cav 3.2 inhibitor 2 (1-10 mg/kg; i.p. 30 min before i.pl. Na2S) affects the Na2S-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: |
| Name | Cav 3.2 inhibitor 2 |
| Formula | C32H37F2N3O |
| Molar Mass | 517.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kasanami Y, et al. Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D2 receptors for treatment of somatic and visceral pain. Eur J Med Chem. 2022 Aug 27;243:114716. |