| Identification | Back Directory | [Name]
DS-1971a | [CAS]
1450595-86-4 | [Synonyms]
DS-1971a
Benzenesulfonamide, 5-chloro-2-fluoro-4-[[(1S,2R)-2-(1-methyl-1H-pyrazol-5-yl)cyclohexyl]oxy]-N-4-pyrimidinyl-
5-Chloro-2-fluoro-4-(((1S,2R)-2-(1-methyl-1H-pyrazol-5-yl)cyclohexyl)oxy)-N-(pyrimidin-4-yl)benzenesulfonamide
hypersensitivity,thermal,Sodium Channel,hyperalgesia,Na channels,inhibit,Na+ channels,Inhibitor,toxicity,DS 1971a,DS-1971a,DS1971a,mechanical | [Molecular Formula]
C20H21ClFN5O3S | [MDL Number]
MFCD32858292 | [MOL File]
1450595-86-4.mol | [Molecular Weight]
465.93 |
| Chemical Properties | Back Directory | [Boiling point ]
638.8±65.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);214.63(Max Conc. mM) | [form ]
Solid | [pka]
3.81±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 vivo]
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.
|
| [IC 50]
hNav1.7: 22.8 nM (IC50); mNav1.7: 59.4 nM (IC50) | [References]
[1] Shinozuka T, et al. Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor [published online ahead of print, 2020 May 26]. J Med Chem. 2020;10.1021/acs.jmedchem.0c00259. DOI:10.1021/acs.jmedchem.0c00259 |
|
|