ChemicalBook > CAS DataBase List > DS-1971a
DS-1971a
- Product Name
- DS-1971a
- CAS No.
- 1450595-86-4
- Chemical Name
- DS-1971a
- Synonyms
- DS-1971a;DS-1971a, 10 mM in DMSO;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;5-chloro-2-fluoro-4-{[(1S,2R)-2-(1-methyl-1H-pyrazol-5-yl)cyclohexyl]oxy}-N-(pyrimidin-4-yl)benzene-1-sulfonamide;hypersensitivity,thermal,Sodium Channel,hyperalgesia,Na channels,inhibit,Na+ channels,Inhibitor,toxicity,DS 1971a,DS-1971a,DS1971a,mechanical
- CBNumber
- CB78065880
- Molecular Formula
- C20H21ClFN5O3S
- Formula Weight
- 465.93
- MOL File
- 1450595-86-4.mol
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DS-1971a Property
- 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)
- pka
- 3.81±0.10(Predicted)
- form
- Solid
- color
- White to off-white
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N-Bromosuccinimide Price
ChemScene
- Product number
- CS-0130195
- Product name
- DS-1971a
- Purity
- 99.66%
- Packaging
- 25mg
- Price
- $1050
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0130195
- Product name
- DS-1971a
- Purity
- 99.66%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0130195
- Product name
- DS-1971a
- Purity
- 99.66%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0130195
- Product name
- DS-1971a
- Purity
- 99.66%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
DC Chemicals
- Product number
- 020465
- Product name
- DS-1971a
- Packaging
- 001
- Price
- $900
- Updated
- 2021/12/16
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DS-1971a Chemical Properties,Usage,Production
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
DS-1971a Preparation Products And Raw materials
Raw materials
Preparation Products
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