A 839977 |
| Catalog No.GC15434 |
P2X7 antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 870061-27-1
Sample solution is provided at 25 µL, 10mM.
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A839977 is a novel and selective antagonist of P2X7 receptor with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively [1].
A839977 has been reported to block BzATP-evoked changes in intracellular calcium concentrations in 132N1 cells stable expressing P2X7 receptors with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively. In addition, A839977 has also revealed to inhibit BzATP-stimulated IL-1β release and YO-PRO uptake with the IC50 of 37nM and 7nM, respectively, in differentiated human THP-1 cells. Besides, A839977 has been noted to produce parallel rightward shifts in BzATP concentration-effect calcium influx curves with the pAα value of 8.1. Apart from these, A839977 has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg(i.p.) [1].
References:
[1] Honore P1, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81.
| Cas No. | 870061-27-1 | SDF | |
| Chemical Name | (E)-N-(1-(2,3-dichlorophenyl)-1H-tetrazol-5(2H)-ylidene)-1-(2-(pyridin-2-yloxy)phenyl)methanamine | ||
| Canonical SMILES | ClC1=C(Cl)C(N2/C(N=NN2)=N\CC3=CC=CC=C3OC4=CC=CC=N4)=CC=C1 | ||
| Formula | C19H14Cl2N6O | M.Wt | 413.26 |
| Solubility | DMSO : 100 mg/mL (241.98 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. |
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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 | 2.4198 mL | 12.0989 mL | 24.1978 mL |
| 5 mM | 0.484 mL | 2.4198 mL | 4.8396 mL |
| 10 mM | 0.242 mL | 1.2099 mL | 2.4198 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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