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DS-1971a

Chemical Structure : DS-1971a

CAS No.: 1450595-86-4

DS-1971a (DS1971a)

Catalog No.: PC-72189Not For Human Use, Lab Use Only.

DS-1971a (DS1971a) is a highly potent, selective NaV1.7 inhibitor with IC50 of 22.8 nM (hNaV1.7) and 59.4 nM (mNaV1.7).

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Biological Activity

DS-1971a (DS1971a) is a highly potent, selective NaV1.7 inhibitor with IC50 of 22.8 nM (hNaV1.7) and 59.4 nM (mNaV1.7).
DS-1971a displays weak inhibitory activity against hNaV1.2 (IC50=1960 nM) and hNaV1.6 (IC50=495 nM), superior selectivity against hNaV1.1 and hNaV1.5 (IC50 values >100 uM).
DS-1971a shows a 10-fold higher potency than PF-05089771 using animal models of neuropathic pain.

Physicochemical Properties

M.Wt 465.928
Formula C20H21ClFN5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-chloro-2-fluoro-4-(((1S,2R)-2-(1-methyl-1H-pyrazol-5-yl)cyclohexyl)oxy)-N-(pyrimidin-4-yl)benzenesulfonamide

References

1. Shinozuka T, et al. J Med Chem. 2020 Sep 24;63(18):10204-10220.

2. Asano D, et al. Xenobiotica. 2021 Sep;51(9):1060-1070.

3. Asano D, et al. Drug Metab Dispos. 2021 Dec 20:DMD-AR-2021-000665.

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