ONO-8539
ONO-8539 is an orally active prostanoid EP1 receptor antagonist with competitive, insurmountable binding and slow receptor dissociation for long-duration inhibition. ONO-8539 modulates afferent nerve function related to bladder activity, inhibits detrusor overactivity-related contractions, decreases nonvoiding contractions and voiding duration, and increases uroflow rate with ATP (HY-B2176)-induced detrusor overactivity. ONO-8539 attenuates acid-induced heartburn symptoms, extends time to first heartburn sensation, and prevents primary hypersensitivity after distal esophageal acidification. ONO-8539 can be used for the research of overactive bladder and gastroesophageal reflux disease.
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- CAS. Nr.: 459842-29-6
- Formel: C25H28N2O5S2
- Molecular Weight:500.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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EP1 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 459842-29-6
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Molecular Weight 500.63
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Formel C25H28N2O5S2
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SMILES
O=C(C1=CC=C(COC2=C(N(S(=O)(C3=NC=CS3)=O)CC(C)C)C=C(CCC4)C4=C2)C(C)=C1)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Chapple CR, et al. Phase II study on the efficacy and safety of the EP1 receptor antagonist ONO-8539 for nonneurogenic overactive bladder syndrome. J Urol. 2014;191(1):253-260. [Content Brief]
[2]. Kondo T, et al. A novel prostanoid EP1 receptor antagonist, ONO-8539, reduces acid-induced heartburn symptoms in healthy male volunteers: a randomized clinical trial. J Gastroenterol. 2017;52(10):1081-1089. [Content Brief]
[3]. Naganawa A, et al. Optimization of sulfonamide derivatives as highly selective EP1 receptor antagonists. Bioorg Med Chem. 2006 Dec 1;14(23):7774-89. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ONO-8539 Related Classifications
HY-182513 Related Classifications
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