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A 839977

Catalog No. T14076Cas No. 870061-27-1
Alias A-839977, A839977

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.

A 839977

A 839977

Purity: 98.01%
Catalog No. T14076Alias A-839977, A839977Cas No. 870061-27-1
A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.
Pack SizePriceAvailabilityQuantity
1 mg$37In Stock
2 mg$52In Stock
5 mg$84In Stock
1 mL x 10 mM (in DMSO)$146In Stock
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Purity:98.01%
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Product Introduction

Bioactivity
Description
A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.
Targets&IC50
P2X7 receptor:150 nM (Mouse), P2X7 receptor:42 nM (Rat), P2X7 receptor:20 nM (Human)
In vitro
A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors (IC50=20-150 nM) and inhibits agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. It has demonstrated efficacy in reducing inflammatory and neuropathic pain in animal models[1]. Pre-treatment with A 839977 (50 nM for 1 hour) significantly prevents the pressure-induced rise of IL-1β priming in optic nerve astrocytes[3].
In vivo
In rats, A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30 mins) dose-dependently reduces thermal hyperalgesia induced by intraplantar administration of complete Freund's adjuvant (CFA)[1].In the CFA model of inflammatory pain in wild-type mice, A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30 mins) elicits robust antihyperalgesia, while it shows no effect in IL-1alphabeta knockout mice[1].Furthermore, A 839977 attenuates dorsal horn neuronal responses in cancer-bearing animals[2].
AliasA-839977, A839977
Chemical Properties
Molecular Weight413.26
FormulaC19H14Cl2N6O
Cas No.870061-27-1
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (193.58 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4198 mL12.0989 mL24.1978 mL120.9892 mL
5 mM0.4840 mL2.4198 mL4.8396 mL24.1978 mL
10 mM0.2420 mL1.2099 mL2.4198 mL12.0989 mL
20 mM0.1210 mL0.6049 mL1.2099 mL6.0495 mL
50 mM0.0484 mL0.2420 mL0.4840 mL2.4198 mL
100 mM0.0242 mL0.1210 mL0.2420 mL1.2099 mL

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