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TAK-259 hydrochloride

Chemical Structure : TAK-259 hydrochloride

CAS No.: 1192347-42-4

TAK-259 hydrochloride (TAK259 hydrochloride)

Catalog No.: PC-61509Not For Human Use, Lab Use Only.

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent and selective human α1D adrenoceptor (α1D-AR) antagonist with Ki of 1.1 nM; displays 200-fold and 800-fold selectivity against α1A- and α1B-AR, respectively; shows antagonistic activity by a bladder strip test in rats with bladder outlet obstruction, ameliorates cystitis-induced urinary frequency in rats.

Other Indication

Phase 1 Discontinued

Physicochemical Properties

M.Wt 410.694
Formula C14H14Cl3N3O3S
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-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide hydrochloride

References

1. Sakauchi N, et al. J Med Chem. 2016 Apr 14;59(7):2989-3002.

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