| Identification | Back Directory | [Name]
A 839977 | [CAS]
870061-27-1 | [Synonyms]
A 839977
ACHEMBLOCK F-4551
1-(2,3-dichlorophenyl)-n-[2-(2-pyridinyloxy)benzyl]-1h-tetrazol-5 -amine
1-(2,3-dichlorophenyl)-N-[(2-pyridin-2-yloxyphenyl)methyl]tetrazol-5-amine
1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]Methyl]-1H-tetrazol-5-aMine
1H-Tetrazol-5-amine, 1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-
1-(2,3-Dichlorophenyl)-N-[[2-[(pyridin-2-yl)oxy]phenyl]methyl]-1H-tetrazol-5-amine
1-(2,3-DICHLOROPHENYL)-N-{[2-(PYRIDIN-2-YLOXY)PHENYL]METHYL}-1H-1,2,3,4-TETRAZOL-5-AMINE
A839977
1-(2,3-dichlorophenyl)-N-{[2-(pyridin-2-yloxy)phenyl]methyl}-1H-1,2,3,4-tetrazol-5-amine | [Molecular Formula]
C19H14Cl2N6O | [MDL Number]
MFCD19690959 | [MOL File]
870061-27-1.mol | [Molecular Weight]
413.26 |
| Chemical Properties | Back Directory | [Boiling point ]
604.9±65.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
solid | [pka]
2.96±0.12(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [Uses]
A 839977 is a selective P2X7 receptor antagonist. | [Biological Activity]
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]. | [in vivo]
A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats[1].
A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice[1].
A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals[3]. | Animal Model: | Male Sprague-Dawley, BALB/c mice and IL-1 (?/?) mice for CFA-induced chronic inflammatory | | Dosage: | 30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice) | | Administration: | Injection; pre-injected 30mins | | Result: | Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1 (?/?) mice. |
| [IC 50]
P2X7 Receptor | [storage]
Store at +4°C | [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. |
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