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A 839977

Name: A 839977
Brand: TargetMol
SKU: T14076
Price: 37 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 98.01%

Catalog No. T14076Alias A-839977, A839977Cas No. 870061-27-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$37	In Stock	In Stock
2 mg	$52	In Stock	In Stock
5 mg	$84	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$146	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.01%

Appearance:Solid

Color:White

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COA LCMS

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].
Synonyms	A-839977, A839977

Chemical Properties

Molecular Weight	413.26
Formula	C₁₉H₁₄Cl₂N₆O
Cas No.	870061-27-1
Smiles	Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1
Relative Density.	1.45 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (193.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.99 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4198 mL	12.0989 mL	24.1978 mL	120.9892 mL
5 mM	0.4840 mL	2.4198 mL	4.8396 mL	24.1978 mL
10 mM	0.2420 mL	1.2099 mL	2.4198 mL	12.0989 mL
20 mM	0.1210 mL	0.6049 mL	1.2099 mL	6.0495 mL
50 mM	0.0484 mL	0.2420 mL	0.4840 mL	2.4198 mL
100 mM	0.0242 mL	0.1210 mL	0.2420 mL	1.2099 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc