Z-VAD-OMe-FMK-Z-Val-Ala-Asp-OMe-FMK-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZ-VAD(OMe)-FMKCat. No.: HY-16658CAS No.: 187389-52-2Synonyms: Z-Val-Ala-Asp(OMe)-FMK分式: CHFNO分量: 467.49Sequence: Z-Val-Ala-Asp(OMe)-FMKSequence Shortening: ZVA-D(OMe)-FMK作靶點: Caspase作通路: Apoptosis儲存式: Powder -80C 2 years-20C 1 y

2、earIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (213.91 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1391 mL 10.6954 mL 21.3908 mL5 mM 0.4278 mL 2.1391 mL 4.2782 mL10 mM 0.2139 mL 1.0695 mL 2.1391 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗

3、動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.35 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. 請依序添加每種溶劑： 10% DMSO 90% (20%

4、SBE-CD in saline)Solubility: 2.5 mg/mL (5.35 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.35 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Z-VAD(OMe)-FMK種可滲透細胞的不可逆 pan-caspase 抑制劑。IC50 & Target Caspase體外研究 Z-VAD(OMe)-FMK is a broad-spectrum caspase inhibitor, has been s

5、hown to inhibit the intracellularactivation of caspase-like proteases. The injection of Z-VAD(OMe)-FMK suppresses the caspase-3 activity inlung tissues, and significantly decreases the number of terminal dUTP nick-end labeling-positive cells 1. Z-VAD(OMe)-FMK is administered intraperitoneally at 1 h

6、our before and 6 hours after SAH. Expression ofcaspase-3 and positive TUNEL is examined as markers for apoptosis. Z-VAD(OMe)-FMK suppressesTUNEL and caspase-3 staining in endothelial cells, decreases caspase-3 activation, reduces BBBpermeability, relieves vasospasm, abolishes brain edema, and improv

7、es neurological outcome 2. Z-VAD(OMe)-FMK is a cell-permeable caspase inhibitor, efficiently blocks cell death induced by SMNdeficiency 3.體內(nèi)研究 The survival rate of mice is prolonged significantly by the injection of Z-VAD(OMe)-FMK. All mice succumbedto LPS within 30 hours. By contrast, the mice trea

8、ted with Z-VAD(OMe)-FMK survive significantly longer and27% of the mice survived more than 7 days 1.PROTOCOLCell Assay 3 PCR products containing coding sequences for the dSMN (forward primer: 5-TAA TAC GAC TCA CTA TAGGG AAG ACG TAC GAC GAG TCG-3; and reverse primer: 5-TAA TAC GAC TCA CTA TAG GG GTG

9、GTGCTG GCT TCT TTC-3; product length, 601bps; bold and italics letters represent T7 promoter sequences)and control Drosophila Presenilin (dPsn) gene (forward primer: 5-TAA TAC GAC TCA CTA TAG GG TGGCT GCT GTC AAT CTC-3; and reverse primer: 5-TAA TAC GAC TCA CTA TAG GG CGA TAG CAA CGCTTC TTG-3; produ

10、ct length: 543bps) are obtained and gel-purified. Double-stranded RNAs (dsRNA) aregenerated by transcription with Ribomax T7 Transcription kit and digested with Rnase-free DNase. ThedsRNA products are ethanol precipitated and annealed by incubation at 65C for 30 min and then slowlyallowed to cool at

11、 room temperature. The annealed dsRNA products are analyzed on a 1% agaorse gel toensure the majority of dsRNA existed as a single band. The dsRNA (2 g) and/or plasmid DNAs (2 g) areintroduced into cells by using Cellfectin. Caspase inhibition is achieved by using 50 M of Z-VAD(OMe)-FMKin the cultur

12、e medium 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 12/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration 12 Mice used in this study are 5- to 6-week-old (20 to 22 g) ICR males. Mice are injected with 30 mg/kg LPSfrom E. co

13、li serotype O111:B4 through the tail vein. A single intravenous injection of Z-VAD(OMe)-FMK (0.25mg) is made 15 minutes before LPS injection, followed by three intravenous injections of Z-VAD(OMe)-FMK(0.1 mg each) per hour. Control mice are injected with the same volume of 1% DMSO in sterile saline.

14、Rats 2Male Sprague-Dawley rats weighing 300 to 350 g are anesthetized with -chloralose (40 mg/kg IP) andurethane (400 mg/kg IP). Animals are intubated, and respiration is maintained with a small animal respirator.Rectal temperature is maintained at 370.5C with a heating pad. The left external caroti

15、d artery is isolatedand a 4.0 monofilament nylon suture is inserted through the internal carotid artery to perforate the middlecerebral artery. SAH is confirmed at autopsy in each rat. Sham-operated rats underwent the sameprocedures except that the suture is withdrawn after resistance is felt. Z-VAD

16、(OMe)-FMK (50 M per 0.3 mL)is injected intraperitoneally at 1 hour before and 6 hours after SAH induction. In vehicle group, ratsunderwent SAH induction and are treated with the same volume of vehicle (DMSO diluted in physiologicalbuffer solution). No treatment is applied in sham-operated animals.MC

17、E has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Cell. 2018 Sep 6;174(6):1477-1491.e19. Nat Commun. 2018 Jan 30;9(1):435. Autophagy. 2019 Jun 16:1-16. Theranostics. 2019 May 31;9(13):3732-3753. Elife. 2017 Dec 12;6. pii: e30590.See more custome

18、r validations on HYPERLINK / www.MedChemEREFERENCES1. Kawasaki M, et al. Protection from lethal apoptosis in lipopolysaccharide-induced acute lung injury in mice by a caspaseinhibitor. Am JPathol. 2000 Aug;157(2):597-603.2. Park S, et al. Neurovascular protection reduces early brain injury after subarachnoid hemorrhage. Stroke. 2004 Oct;35(10):2412-7.3. Ilangovan R, et al. Inhibition of apoptosis by