ADRA1D receptor antagonist 1 free base
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
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- CAS No.: 1191908-24-3
- Formula: C15H13ClN4O
- Molecular Weight:300.74
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
ADRA1D receptor antagonist 1 (free base) (4.4 µg/kg; i.v.; single) inhibits bladder contraction with an IC 30 value of 15 nM in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with cyclophosphamide-induced cystitis[1].
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Dosage:10 µg/kg
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Administration:Oral administration; single
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Result:Increased voiding intervals.
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Animal Model:Rats with BOO (bladder outlet obstruction)[1].
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Dosage:4.4 µg/kg
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Administration:Intravenous injection; single
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Result:Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.
Chemical Information
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CAS No. 1191908-24-3
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Molecular Weight 300.74
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Formula C15H13ClN4O
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SMILES
O=C(C1=CC(Cl)=CN([C@@H](C2=CC=CC(C#N)=C2)C)C1=N)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADRA1D receptor antagonist 1 free base Related Classifications
HY-148252 Related Classifications
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