SR 49059 is a potent and selective Arginine Vasopressin (AVP) V1a-receptor antagonist, with a Ki vaule of 1.4 nM. AVP is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes V1a, V1b, and V2. All belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF. SR 49059 has also shown initial positive results in the treatment of Raynaud′s disease, dysmenorrhoea, and tocolysis.
| Molecular Weight | 620.5 |
| Formula | C28H27Cl2N3O7S |
| CAS Number | 150375-75-0 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | -20°C, sealed |
| 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 |
|---|
| d[Cha4]-AVP
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. |
| [Asu1, 6-Arg8]Vasopressin
[Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture. |
| Big Endothelin-1 (1-39), porcine
Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. |
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