TAK-259
TAK-259 is an orally active α1D-adrenergic receptor antagonist with a Ki 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.
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- CAS No.: 1192348-73-4
- 화학식: C14H13Cl2N3O3S
- 분자량:374.24
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
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Alpha-1D adrenergic receptor 1.1 nM (Ki) |
In Vitro
TAK-259 (Compound 9u) (60 min) potently binds to human α1D-adrenergic receptor in a cell membrane-free binding assay, with a Ki 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.
In Vivo
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.
Chemical Information
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CAS No. 1192348-73-4
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분자량 374.24
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화학식 C14H13Cl2N3O3S
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SMILES
O=C(C1=CC(Cl)=CN(CC2=CC(Cl)=CC=C2S(=O)(C)=O)C1=N)N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAK-259 Related Classifications
HY-120473 Related Classifications
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