الصفحة الرئيسية>>Signaling Pathways>> Proteases>> Elastase>>ZD-0892

ZD-0892

رقم الكتالوجGC32628

ZD-0892 هو مثبط انتقائي وقوي لإيلاستاز العدلات مع Kis من 6.7 و 200 نانومتر للإيلاستاز العدلات البشرية والإيلاستاز البنكرياس الخنازير ، على التوالي

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ZD-0892 التركيب الكيميائي

Cas No.: 171964-73-1

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Sample solution is provided at 25 µL, 10mM.

Description of ZD-0892

ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.

ZD0892 administration to DBA/2 mice infected with the EMC virus results in reduced myocardial elastolytic activity and coronary microvascular perfusion injury. ZD0892 decreases the pathologic severity of the myocardial lesions associated with murine viral myocarditis[1]. ZD-0892 can reverse advanced pulmonary vascular disease produced in rats[2].

[1]. Lee JK, et al. A serine elastase inhibitor reduces inflammation and fibrosis and preserves cardiac function after experimentally-induced murine myocarditis. Nat Med. 1998 Dec;4(12):1383-91. [2]. Cowan KN, et al. Complete reversal of fatal pulmonary hypertension in rats by a serine elastase inhibitor. Nat Med. 2000 Jun;6(6):698-702.

Protocol of ZD-0892

Animal experiment:

Rats[2]Adult male Sprague-Dawley rats (250-300 g in body weight) are induced pulmonary hypertension. In addition to a group of untreated rats, the experimental groups include rats that receive twice-daily gavage tube feedings of ZD0892, at a dose of 240 mg/kg per day or vehicle (5% polyethylene glycol or dimethyl sulfoxide). Rats are examined after 7 days of treatment.Mice[1]DBA/2 male mice 8 weeks old is used. ZD0892 is given in a dose of 60 mg/kg or 120 mg/kg[1].

References:

[1]. Lee JK, et al. A serine elastase inhibitor reduces inflammation and fibrosis and preserves cardiac function after experimentally-induced murine myocarditis. Nat Med. 1998 Dec;4(12):1383-91.
[2]. Cowan KN, et al. Complete reversal of fatal pulmonary hypertension in rats by a serine elastase inhibitor. Nat Med. 2000 Jun;6(6):698-702.

Chemical Properties of ZD-0892

Cas No. 171964-73-1 SDF
Canonical SMILES CC(C)[C@@H](C(N1[C@H](C(N[C@H](C(C(F)(F)F)=O)C(C)C)=O)CCC1)=O)NC(C2=CC=C(OC)C=C2)=O
Formula C24H32F3N3O5 M.Wt 499.52
الذوبان DMSO : 250 mg/mL (500.48 mM; Need ultrasonic) 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 of ZD-0892

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0019 mL 10.0096 mL 20.0192 mL
5 mM 0.4004 mL 2.0019 mL 4.0038 mL
10 mM 0.2002 mL 1.001 mL 2.0019 mL
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In vivo Formulation Calculator (Clear solution) of ZD-0892

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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