Name | 6-[2-(6-Hydroxy-heptyl)-thiazol-4-yl]-4,5-dimethoxy-pyridine-2-carboxylic acid |
---|---|
Synonyms | (±)-WS75624B |
Description | (±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL. |
---|---|
Related Catalog | |
Target |
IC50: 0.03 μg/mL (ECE)[1] |
In Vitro | Endothelin converting enzyme (ECE) inhibitors, WS75624A and (±)-WS75624B, have been isolated from the fermentation broth of Saccharothrix sp. No. 75624. WS75624A and (±)-WS75624B show highly potent ECE inhibitory activity, and both have IC50s of 0.03 μg/mL. WS75624A and (±)-WS75624B also show other metalloprotease (collagenase and neutral endopeptidase) inhibitory activity with IC50 s of 1 μg/mL. (±)-WS75624B markedly inhibits ECE activity with an IC50 value of 0.03 μg/mL, while it weakly inhibit collagenase and NEP activities with IC50s of 1.0 μg/mL and 1.25 μg/mL, respectively[1]. |
In Vivo | (±)-WS75624B inhibits big endothelin-induced pressor effect when administered to SD rat intravenously with big ET-1. WS75624 B (30 mg/kg) markedly attenuates the hypertensive effect of big ET-1 (1 nmol/kg,iv) the inhibiting the conversion of big ET-1 to ET-1[1]. |
Animal Admin | Rats[1] Male Sprague-Dawley rats (250-300 g) are anesthetized with Pentobarbital sodium (50 mg/kg of boby weight). A femoral artery catheter is implanted for monitoring arterial pressure and heart rate, and a femoral vein catheter is used for injection of saline or drugs. Blood pressure and heart rate is recorded from the femoral artery through a cannula (PE-50) connected to a pressure transducer coupled to a Biophysiograph RM 6000 system. Two groups of rats are injected with the following: Big ET-1 (1 nmol/kg) alone (n=7), big ET-1 (1 nmol/kg) with (±)-WS75624B (30 mg/kg) iv bolus injection (n=7). |
References |
Molecular Formula | C18H24N2O5S |
---|---|
Molecular Weight | 380.45900 |
Exact Mass | 380.14100 |
PSA | 130.01000 |
LogP | 3.40420 |