TAK-259 hydrochloride 

TAK-259 hydrochloride is an orally active α1D-adrenergic receptor antagonist with a K_i value of 1.1 nM for human α1D-adrenergic receptors. TAK-259 hydrochloride 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 hydrochloride can be used in research related to overactive bladder^[1].

TAK-259 (Compound 9u) (60 min) hydrochloride 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) hydrochloride 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.) hydrochloride 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.) hydrochloride 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.

410.70

C₁₄H₁₄Cl₃N₃O₃S

1192347-42-4

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. 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]