| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GW-791343 3HCl, the trihydrochloride salt form of GW-791343 (GW791343) is a novel, potent P2X7 allosteric modulator that exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 with pIC50 of 6.9 - 7.2. GW791343 is a positive allosteric modulator of rat P2X7.
| ln Vitro |
At the human P2X7 receptor, GW791343 diHClide (0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM; 40 min) exhibits non-competitive antagonistic action [1]. On the human P2X7 receptor, GW791343 diHClide (3, 10, 30 µM; 40 minutes) has negative allosteric modulatory action [1]. SCN cells' ATP rhythms are improved by GW791343 diHClide (5 µM; 24-48 hours; ATP measured every 4 hours) [2].
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| Cell Assay |
Cell viability assay[1]
Cell Types: HEK293 cells (expressing human recombinant P2X7 receptor) Tested Concentrations: 3, 10, 30 µM Incubation Duration: 40 minutes (10 minutes of pre-incubation, 30 minutes of incubation with other P2X7 receptor antagonists) Experimental Results: demonstrated slow reversal of human P2X7 receptor (full reversal after 45 minutes) with fast dissociation rate. Cell viability assay[2] Cell Types: SCN cells (from 16 to 21 day old Wistar rats maintained under a controlled 12-12 hour light/dark cycle from birth) Tested Concentrations: 5 µM (used every 4 hrs (hours) fresh medicated culture medium). Incubation Duration: 24-48 hrs (hours) (ATP measured every 4 hrs (hours)) Experimental Results: The amplitude of ATP release rhythm and extracellular ATP accumulation was enhanced to 144% of the control level. |
| References |
| Molecular Formula |
C20H24N4OF2.HCL
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|---|---|
| Molecular Weight |
410.8885
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| Exact Mass |
446.145
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| CAS # |
1019779-04-4
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| Related CAS # |
GW791343 trihydrochloride;309712-55-8
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| PubChem CID |
71576670
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| Appearance |
White to off-white solid powder
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| LogP |
5.547
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
475
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IYJPZTBIYHPSKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24F2N4O.2ClH/c1-14-2-3-15(13-26-8-6-23-7-9-26)10-19(14)25-20(27)12-24-16-4-5-17(21)18(22)11-16;;/h2-5,10-11,23-24H,6-9,12-13H2,1H3,(H,25,27);2*1H
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| Chemical Name |
2-(3,4-difluoroanilino)-N-[2-methyl-5-(piperazin-1-ylmethyl)phenyl]acetamide;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~223.54 mM)
DMSO : ~20 mg/mL (~44.71 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (4.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (111.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4337 mL | 12.1687 mL | 24.3374 mL | |
| 5 mM | 0.4867 mL | 2.4337 mL | 4.8675 mL | |
| 10 mM | 0.2434 mL | 1.2169 mL | 2.4337 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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