Shanghai Nianxing Industrial Co., Ltd
China
Product Name: (±)-WS75624B
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Purity: 98.0%
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188048-45-5

188048-45-5 structure

188048-45-5 structure

Name: (±)-WS75624B
Chemical Name: 6-[2-(6-Hydroxy-heptyl)-thiazol-4-yl]-4,5-dimethoxy-pyridine-2-carboxylic acid
CAS Number: 188048-45-5
Molecular Formula: C₁₈H₂₄N₂O₅S
Molecular Weight: 380.45900
Catalog: Research Areas Cardiovascular Disease
Create Date: 2017-05-16 04:44:54
Modify Date: 2024-01-04 21:45:39
(±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL.

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	Signaling Pathways >> Others >> Others Research Areas >> Cardiovascular Disease
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	[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):1066-72.

Molecular Formula	C₁₈H₂₄N₂O₅S
Molecular Weight	380.45900
Exact Mass	380.14100
PSA	130.01000
LogP	3.40420

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