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(±)-WS75624B Sale

目录号 : GC32617

(±)-WS75624B是一种内皮素转化酶(ECE)抑制剂,IC50为0.03μg/mL。

(±)-WS75624B Chemical Structure

Cas No.:188048-45-5

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1mg
¥23,473.00
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5mg
¥37,556.00
现货
10mg
¥60,092.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Animal experiment:

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.

产品描述

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

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].

(±)-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].

[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.

Chemical Properties

Cas No. 188048-45-5 SDF
Canonical SMILES O=C(C1=NC(C2=CSC(CCCCCC(O)C)=N2)=C(OC)C(OC)=C1)O
分子式 C18H24N2O5S 分子量 380.46
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6284 mL 13.142 mL 26.284 mL
5 mM 0.5257 mL 2.6284 mL 5.2568 mL
10 mM 0.2628 mL 1.3142 mL 2.6284 mL
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