GK241 |
| Katalog-Nr.GC52315 |
An sPLA2 (Type IIA) inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1899930-93-8
Sample solution is provided at 25 µL, 10mM.
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GK241 is a secretory phospholipase A2 (sPLA2) (Type IIA) inhibitor (IC50s = 0.143 and 0.068 µM for the human and mouse enzymes, respectively).1,2 It inhibits IL-1β-induced production of prostaglandin E2 in isolated rat renal mesangial cells when used at concentrations of 3 and 10 µM.3 GK241 also inhibits the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro; IC50 = 24 µM).1
1.Theodoropoulou, M.A., Koutoulogenis, G.S., Zhang, L., et al.Identification of a dual inhibitor of secreted phospholipase A2 (GIIA sPLA2) and SARS-CoV-2 main proteasePharmaceuticals (Basel)15(8)961(2021) 2.Vasilakaki, S., Barbayianni, E., Leonis, G., et al.Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulationsBioorg. Med. Chem.24(8)1683-1695(2016) 3.Vasilakaki, S., Barbayianni, E., Magrioti, V., et al.Inhibitors of secreted phospholipase A2 suppress the release of PGE2 in renal mesangial cellsBioorg. Med. Chem.24(13)3029-3034(2016)
| Cas No. | 1899930-93-8 | SDF | |
| Canonical SMILES | CCCCCCCCCCCCCCC(C(N[C@H](C(O)=O)C(C)C)=O)=O | ||
| Formula | C21H39NO4 | M.Wt | 369.5 |
| Löslichkeit | DMF: slightly soluble,DMSO: 2 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): insol | Storage | -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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7064 mL | 13.5318 mL | 27.0636 mL |
| 5 mM | 0.5413 mL | 2.7064 mL | 5.4127 mL |
| 10 mM | 0.2706 mL | 1.3532 mL | 2.7064 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 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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