Biological Activity
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects[1].
In Vitro
DS-1971a exhibits a favorable toxicological profile[1]. DS-1971a (0.1-1 mg/kg; p.o.) shows mitigated thermal hyperalgesia in a dose-dependent manner in partial sciatic nerve ligation (PSL) mice[1]. Animal Model: Male Slc:ddY mice (PSL model)[1] Dosage: 0.1, 0.3, and 1 mg/kg Administration: P.o. Result: A significant dose-dependent suppression of thermal hyperalgesiain 0.3 and 1 mg/kg administered groups. The ED50 of DS-1971a at the peak efficacy was 0.32 mg/kg.
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
References & source
1: Tsuyoshi Shinozuka, Hiroyuki Kobayashi, Sayaka Suzuki, Kyosuke Tanaka, Narayan Karanjule, Noriyuki Hayashi, Toshifumi Tsuda, Eri Tokumaru, Masahiro Inoue, Kiyono Ueda, Hiroko Kimoto, Yuki Domon, Sakiko Takahashi, Kazufumi Kubota, Tomihisa Yokoyama, Aki
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.