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GW791343 3HCl
CAS No. 309712-55-8
GW791343 3HCl( —— )
Catalog No. M17471 CAS No. 309712-55-8
GW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 65 | Get Quote |
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| 10MG | 111 | Get Quote |
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| 25MG | 199 | Get Quote |
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| 100MG | 768 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameGW791343 3HCl
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NoteResearch use only, not for human use.
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Brief DescriptionGW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
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DescriptionGW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
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In VitroGW791343 trihydrochloride (0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 40 min) shows a non-competitive antagonistic activity to the human P2X7 receptor.GW791343 trihydrochloride (3, 10, 30 μM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor.GW791343 trihydrochloride (5 μM; 24-48 h; ATP measured every 4 h) enhances ATP rhythm in SCN cells. Cell Viability Assay Cell Line:HEK293 cells (expressing human recombinant P2X7 receptors).Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM.Incubation Time:40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min).Result:Inhibited agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer.Reduced maximal responses toATP and BzATP in sucrose buffer.Cell Viability Assay Cell Line:HEK293 cells (expressing human recombinant P2X7 receptors).Concentration:3, 10, 30 μM.Incubation Time:40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min).Result:Showed slow reversal effects at the human P2X7 receptor (after 45 min had reversed sufficiently), and had a rapid dissociation rate.Cell Viability Assay Cell Line:SCN cells (from 16-to 21- day-old Wistar rats, which are kept under a controlled 12-12 h light-dark cycle from birth).Concentration:5 μM (replace the medium with fresh drug-containing culture medium every 4 h).Incubation Time:24-48 h (ATP measured every 4 h).Result:Enhanced the amplitude of ATP release rhythm and extracellular ATP accumulation to 144 of control levels.
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In Vivo——
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Synonyms——
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PathwayNeuroscience
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TargetGluR
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RecptorP2X7
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number309712-55-8
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Formula Weight483.81
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Molecular FormulaC20H24F2N4O·3HCl
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Purity>98% (HPLC)
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Solubility——
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SMILESCC1=C(C=C(C=C1)CN2CCNCC2)NC(=O)CNC3=CC(=C(C=C3)F)F.Cl.Cl.Cl
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Dipraglurant
Dipraglurant (ADX48621) is a negative alteration modulator (NAM) of mGluR5 that inhibits dyskinesia in the LID macaque model.
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VU6012962
VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).
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Basimglurant
Basimglurant is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM).
