TAK 259

• CAT Number: I009685
• CAS Number: 1192347-42-4
• Molecular Formula: C14H13Cl2N3O3S.HCl
• Molecular Weight: 410.7
• Purity: ≥95%
• IUPAC Name: 5-chloro-1-[(5-chloro-2-methylsulfonylphenyl)methyl]-2-iminopyridine-3-carboxamide;hydrochloride
• InChI: InChI=1S/C14H13Cl2N3O3S.ClH/c1-23(21,22)12-3-2-9(15)4-8(12)6-19-7-10(16)5-11(13(19)17)14(18)20;/h2-5,7,17H,6H2,1H3,(H2,18,20);1H
• SMILES: CS(=O)(=O)C1=C(C=C(C=C1)Cl)CN2C=C(C=C(C2=N)C(=O)N)Cl.Cl

Novel, selective, and orally active α1D adrenoceptor antagonist (Ki value 1.1 nM, and 200-800 fold selective over α1A and α1B, respectively) with anti-urinary frequency effects: reducing human Ether-a-go-go-Related Gene (hERG) liabilities. Clinical candidate, and a promising novel therapeutic agent for the treatment of OAB (overactive bladder) symptoms.
KEYWORDS: TAK 259 | supplier | α1D antagonist | TAK259 | CAS [1192347-42-4] | [1192348-73-4] | Adrenaline | Adrenoceptor α1 | GPCR | anti-urinary | hERG liabilities | human Ether-a-go-go-Related Gene | overactive bladder | OAB

Reference

N Sakauchi et al. Discovery of TAK-259 as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. J Med Chem. 2016 Apr 14;59(7):2989-3002.