MX1013 (Synonyms: Z-Val-Asp-Fluoromethyl Ketone, Z-VD-FMK) |
カタログ番号GC45515
One-Click Copy Product Info
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MX1013 は、抗アポトーシス活性を持つ、強力で不可逆的なジペプチド カスパーゼ阻害剤です。 MX1013 は、30 nM の IC50 で組換えヒトカスパーゼ 3 を阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 582316-00-5
Sample solution is provided at 25 µL, 10mM.
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MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1 (IC50 = 20 nM), caspase-3 (IC50 = 30 nM), and caspase-6, -7, -8, and -9 (IC50s = 5-18 nM).1 It is selective for caspases over calpain I, cathepsin B, cathepsin D, renin, thrombin, and Factor Xa (IC50s = >10 μM). MX1013 (0.05 μM) inhibits anti-Fas antibody-induced caspase-3 processing and poly(ADP)ribose polymerase (PARP) cleavage in Jurkat cells, indicating inhibition of apoptosis. It increases survival in a mouse model of anti-Fas antibody-induced liver failure when administered at doses of greater than or equal to 0.25 mg/kg. MX1013 reduces infarct size in rat models of acute myocardial infarction-reperfusion or transient focal brain ischemia-reperfusion injury when administered intravenously as a 20 mg/kg bolus dose followed by a 5 mg/kg per hour infusion.
References
1. Yang, W., Guastella, J., Huang, J.-C., et al. MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity. Br. J. Pharmacol. 140(2), 402-412 (2003).
| Cas No. | 582316-00-5 | SDF | |
| 同義語 | Z-Val-Asp-Fluoromethyl Ketone, Z-VD-FMK | ||
| Canonical SMILES | O=C(O)CC(NC([C@@H](NC(OCC1=CC=CC=C1)=O)C(C)C)=O)C(CF)=O | ||
| Formula | C18H23FN2O6 | M.Wt | 382.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 10 mg/ml | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6151 mL | 13.0753 mL | 26.1506 mL |
| 5 mM | 523 μL | 2.6151 mL | 5.2301 mL |
| 10 mM | 261.5 μL | 1.3075 mL | 2.6151 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)