GSK199 (hydrochloride) |
| رقم الكتالوجGC43789 |
GSK199 (هيدروكلوريد) هو مثبط PAD4 قابل للانعكاس وانتقائي مع IC50 من 200 نانومتر في حالة عدم وجود الكالسيوم.
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Cas No.: 1549811-53-1
Sample solution is provided at 25 µL, 10mM.
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Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases. GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.It is less potent than the related PAD4 inhibitor GSK484 , which demonstrates an IC50 value of 50 nM. GSK199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.
| Cas No. | 1549811-53-1 | SDF | |
| Canonical SMILES | N[C@H]1CN(C(C2=CC(N=C(C3=CC(C=CC=N4)=C4N3CC)N5C)=C5C(OC)=C2)=O)CCC1.Cl | ||
| Formula | C24H28N6O2•HCl | M.Wt | 469 |
| الذوبان | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 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 | 2.1322 mL | 10.661 mL | 21.322 mL |
| 5 mM | 0.4264 mL | 2.1322 mL | 4.2644 mL |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1322 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 37 reference(s) in Google Scholar.)
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