DS-1971a

Research use only, not for human use.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.(In Vitro):DS-1971a showed high NaV1.7 inhibitory potency in vitro. The IC50 values are of 22.8 nM for hNaV1.7 and 59.4 mM for mNaV1.7.(In Vivo):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 with ED50 of 0.32 mg/kg.

——

DS-1971a exhibits a favorable toxicological profile.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. Animal Model:Male Slc:ddY mice (PSL model)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.

——

Membrane Transporter/Ion Channel

Sodium Channel

AChE

——

——

1450595-86-4

465.93

C20H21ClFN5O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (214.62 mM)

Cn1nccc1[C@@H](CCCC1)[C@H]1Oc(cc(c(S(Nc1ncncc1)(=O)=O)c1)F)c1Cl

——

(-20℃)

With Ice Pack

≥ 2 years