Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
| Molecular Weight | 518.65 |
| Formula | C30H38N4O4 |
| CAS Number | 872599-83-2 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Oxytocin Receptor Products |
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| [Asp5]-Oxytocin
[Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. |
| (d(CH2)51, Tyr(Me)2, Thr4, Orn8, Tyr-NH29)-Vasotocin
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,Tyr-NH29)-Vasotocin is an oxytocin antagonist and can be used for the research of sexual behavior. |
| (d(CH2)51, Tyr(Me)2, Orn8)-Oxytocin
(d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist. |
| (Val3, Pro8)-Oxytocin
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. |
| (d(CH2)51, Tyr(Me)2, Thr4, Orn8, des-Gly-NH29)-Vasotocin
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, an oxytocin receptor antagonist, abolishes oxytocin-enhanced inhibitory postsynaptic currents in CA1 pyramidal neurons. |
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