Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. Bosentan (BOS) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. The in vitro binding affinity of Bosentan to ETA receptors on human SMC is 4.7 nM and to ETB receptors on human SMC or placenta cells is 41 or 95 nM.
| Molecular Weight | 551.61 |
| Formula | C27H29N5O6S |
| CAS Number | 147536-97-8 |
| Solubility (25°C) | DMSO 80 mg/mL |
| 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 Endothelin Receptor Products |
|---|
| Endothelin 1 (swine, human) (TFA)
Endothelin 1 (swine, human) (TFA) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. |
| Atrial Natriuretic Peptide (ANP) (1-28), rat
Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner. |
| [Asn18] Endothelin-1, human
[Asn18] Endothelin-1, human is a peptide. |
| [Lys4] Sarafotoxin S6c
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. |
| [Ala2] Endothelin-3, human
[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. |
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