Bioactivity | (±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL. |
Target | IC50: 0.03 μg/mL (ECE) |
Invitro | 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]. |
Name | (±)-WS75624B |
CAS | 188048-45-5 |
Formula | C18H24N2O5S |
Molar Mass | 380.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Tsurumi Y, et al. WS75624 A and B, new endothelin converting enzyme inhibitors isolated from Saccharothrix sp. No. 75624. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1995 Oct;48(10):1066 |