TAK-259 

TAK-259 is an orally active α1D-adrenergic receptor antagonist with a K_i value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 can inhibit the contraction of isolated bladder strips in rats with bladder outlet obstruction, reduce non-voiding bladder contractions, and improve urinary frequency symptoms. TAK-259 can be used in research related to overactive bladder^[1].

TAK-259 (Compound 9u) (60 min) potently binds to human α₁D-adrenergic receptor in a cell membrane-free binding assay, with a K_i value of 1.1 nM^[1].
TAK-259 (10 μM; 5 min at 32°C) exhibits low inhibitory activity against hERG K⁺ channels in cell-based patch-clamp assays (16% inhibition at 10 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-259 (i.v.) reduces non-voiding bladder contractions in rats with bladder outlet obstruction in a dose-dependent manner, with an IC₃₀ of 12 nM and an ID₅₀ of 1.3 µg/kg^[1].
TAK-259 (10 µg/kg; p.o.) reduces micturition frequency in Cyclophosphamide (HY-17420)-induced cystitis rats when administered at the minimum effective dose of 10 µg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

374.24

C₁₄H₁₃Cl₂N₃O₃S

1192348-73-4

O=C(C1=CC(Cl)=CN(CC2=CC(Cl)=CC=C2S(=O)(C)=O)C1=N)N

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sato A, et al. Structure determination, synthesis, and biological evaluation of a metabolite of the selective α1D adrenoceptor antagonist TAK-259[J]. Tetrahedron, 2016, 72(41): 6334-6339.

  [2]. Sakauchi N, et al. Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (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.  [Content Brief]