L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Decreases length of U-87MG cell projections induced by retinoic acid (Cat.No.0695). Orally active.
| Molecular Weight | 507.59 |
| Formula | C28H33N3O6 |
| CAS Number | 162042-44-6 |
| Solubility (25°C) | DMSO 5.08 mg/mL (with gentle warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Vasopressin Receptor Products |
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d[Cha4]-AVP is a potent and selective vasopressin (AVP) V1b receptor agonist with a Ki of 1.2 nM for human V1b receptor. |
| Big Endothelin-1 (1-38), human
Big Endothelin-1 (1-38), human is the precursor of endothelin-1. |
| (d(CH2)51, Tyr(Me)2, Arg8)-Vasopressin
(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin (SKF 100273) is a vasopressin V1 receptor selective antagonist. |
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| Big Endothelin-1 (1-39), porcine
Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. |
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