Powder: -20°C for 3 years | In solvent: -80°C for 1 year
OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 80,500 |
5 mg | 在庫あり | ¥ 190,000 |
10 mg | 在庫あり | ¥ 259,500 |
25 mg | 在庫あり | ¥ 365,000 |
50 mg | 在庫あり | ¥ 454,500 |
100 mg | 在庫あり | ¥ 574,000 |
500 mg | 在庫あり | ¥ 1,124,500 |
説明 | OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia. |
ターゲット&IC50 | V2 receptor:91.9+10.8 nM(Ki), cAMP:189+/-14 nM(EC50), V2 receptor:189+14 Nm(EC50), V1a receptor:819+39 nM(Ki) |
In vitro |
OPC-51803 and dDAVP displaced [(3)H]-AVP binding to human V(2)- and V(1a)-receptors with K(i) values of 91.9+/-10.8 nM (n = 6) and 3.12+/-0.38 nM (n = 6) for V(2)-receptors, and 819+/-39 nM (n = 6) and 41.5+/-9.9 nM (n = 6) for V(1a)-receptors, indicating that OPC-51803 was about nine times more selective for V(2)-receptors, similar to the selectivity of dDAVP.[5] OPC-51803 concentration-dependently increased cyclic adenosine 3', 5'-monophosphate (cyclic AMP) production in HeLa cells expressing human V(2)-receptors with an EC(50) value of 189+/-14 nM (n = 6).[5] |
In vivo |
OPC-51803 shows antidiuretic action in dogs. OPC-51803 (0.03 to 0.3 mg/kg; oral) decreased urine volume and increased urinary osmolality in a dose-dependent manner in water-loaded dogs.[4] OPC-51803 infusions (0.3 and 3 microg x kg(-1) x min(-1); Intravenous ) did not affect renal or systemic hemodynamics in anesthetized dogs.[4] |
別名 | SOU-003, SOU 003, SOU003, OPC51803, OPC 51803 |
分子量 | 454 |
分子式 | C26H32ClN3O2 |
CAS No. | 192514-54-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (99.12 mM)
You can also refer to dose conversion for different animals. 詳細
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OPC-51803 192514-54-8 GPCR/G Protein Vasopressin Receptor SOU-003 SOU 003 SOU003 OPC51803 OPC 51803 Inhibitor inhibitor inhibit