Name | A-804598 |
Synonyms | CS-2234 A 804598 A-804598 1-cyano-2-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine 1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE 2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine Guanidine, N-cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl- |
CAS | 1125758-85-1 |
Molecular Formula | C19H17N5 |
Molar Mass | 315.37 |
Density | 1.17±0.1 g/cm3(Predicted) |
Boling Point | 498.0±47.0 °C(Predicted) |
Solubility | DMSO: ≥ 32 mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 4.52±0.12(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
In vitro study | Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity. Cell Cytotoxicity Assay Cell Line: microglial cell Concentration: 0.1, 0.3, 1, 3, 10 μM Incubation Time: 1 hour Result: Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia. |
In vivo study | A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease. Animal Model: Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice Dosage: 30 mg/kg Administration: Intraperitoneal injection; five times a week Result: Decreased SQSTM1/p62 expression. |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.171 ml | 15.854 ml | 31.709 ml |
5 mM | 0.634 ml | 3.171 ml | 6.342 ml |
10 mM | 0.317 ml | 1.585 ml | 3.171 ml |
5 mM | 0.063 ml | 0.317 ml | 0.634 ml |
biological activity | A-804598 is a CNS penetrating, competitive and selective P2X7 receptor antagonist that acts in mice, the rat and human P2X7 receptors, IC50s, are 9 nM, 10 nM and 11 nM, respectively. |
Target | IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor) |
in vitro study | Pre-incubation with A- 804598 (0.1-10 μm; 1 hour) significant attributes BzATP-induced cell loss in a concentration-dependent manner. 3 μm A- 804598 exhibits the great protective effect against BzATP-induced Cytoxicity. Cell cytotoxity Assay Cell Line: microglial cell Concentration: 0.1, 0.3, 1, 3, 10 μM Incubation Time: 1 hour Result: Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia. |
Cell Line: | microglial cell |
Concentration: | 0.1, 0.3, 1, 3, 10 μM |
Incubation Time: | 1 hour |
Result: | Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia. Decreased SQSTM1/p62 expression. |
in vivo study | A pH treatment with A- 804598 (intraperone injection; 30 mg/kg; five times a week) the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease. Animal Model: Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice Dosage: 30 mg/kg; five times a week Result: Decreased SQSTM1/p62 expression. |
Animal Model: | Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice |
Dosage: | 30 mg/kg |
Administration: | Intraperitoneal injection; five times a week |