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TAK 259
- Parent CAS: 1192348-73-4
- Soluble in water and DMSO
- MF: C14H13Cl2N3O3S.HCl
- MW: 410.7
Description
TAK 259 is a potent, selective, and orally active α1D adrenoceptor antagonist (Ki = 1.1 nM) with 200-800 fold selectivity over α1A and α1B receptors. It demonstrates strong anti-urinary frequency effects with reduced hERG channel liability, making it a clinical candidate for the treatment of OAB (overactive bladder) symptoms.
α1D pharmacology is relevant to disease-relevant cellular and translational research models; TAK 259 supports mechanistic studies of α1D-adrenoceptor across biochemical, cellular and disease-model assays.
Key Features
- Potent and orally active α1D antagonist (Ki = 1.1 nM)
- 200-800 fold selective over α1A and α1B subtypes
- Modulates α1D-dependent signaling or biological activity
- Clinical candidate for the treatment of OAB symptoms
Applications
- α1D pharmacology and target-validation studies
- α1D pathway and signaling assays
- Disease-relevant cellular and translational model systems
- Receptor signaling, ligand profiling and functional response assays
More Information
| Parent CAS No. | 1192348-73-4 |
|---|---|
| Chemical Name | 5-chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide hydrochloride |
| SMILES | C1(=N)N(CC2=CC(Cl)=CC=C2S(C)(=O)=O)C=C(Cl)C=C1C(N)=O.Cl |
| MFCD | N.A. |
| 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 |
| InChiKey | MWQYDDZQXFWUAN-UHFFFAOYSA-N |
| CID | 66970086 |
| Short Description | α1D antagonist |
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