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(±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL.

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(±)-WS75624B Chemical Structure

(±)-WS75624B Chemical Structure

CAS No. : 188048-45-5

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Description

(±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL.

IC50 & 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

380.46

Formula

C18H24N2O5S

CAS No.
SMILES

O=C(C1=NC(C2=CSC(CCCCCC(O)C)=N2)=C(OC)C(OC)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
Animal Administration
[1]

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).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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(±)-WS75624B Related Classifications

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Product Name:
(±)-WS75624B
Cat. No.:
HY-100312
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