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(±)-WS75624B

Katalog-Nr.GC32617

(±)-WS75624B ist ein Inhibitor des Endothelin-Converting-Enzyms (ECE) mit einem IC50-Wert von 0,03 μg/ml.

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(±)-WS75624B Chemische Struktur

Cas No.: 188048-45-5

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.

Background

(±)-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
Formula C18H24N2O5S M.Wt 380.46
Löslichkeit Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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