A 839977
Modify Date: 2024-01-02 18:32:04
A 839977 structure
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Common Name | A 839977 | ||
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| CAS Number | 870061-27-1 | Molecular Weight | 413.26000 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C19H14Cl2N6O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of A 839977A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).IC50 Value: Target: P2X7in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1]. |
| Name | 1-(2,3-Dichlorophenyl)-N-[2-(2-pyridinyloxy)benzyl]-1H-tetrazol-5 -amine |
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| Synonym | More Synonyms |
| Description | A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).IC50 Value: Target: P2X7in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1]. |
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| Related Catalog | |
| References |
| Molecular Formula | C19H14Cl2N6O |
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| Molecular Weight | 413.26000 |
| Exact Mass | 412.06100 |
| PSA | 80.98000 |
| LogP | 4.19040 |
| A 839977 |