A-286501 | CAS 483341-15-7

A-286501

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Cat #: V3081 CAS #: 483341-15-7 Purity ≥ 98%

Description: A-286501 is a novel and potent carbocyclic nucleoside AK (Adenosine kinase) inhibitor with an IC50 of 0.47 nM and has analgesic and anti-inflammatory activities. It has no significant activity (IC50 >100 microM) at other sites of ADO (Adenosine) interaction (A1, A2A, A3 receptors, ADO transporter, and ADO deaminase) or other (IC50 value >10 microM) neurotransmitter and peptide receptors, ion channel proteins, neurotransmitter reuptake sites and enzymes, including cyclooxygenases-1 and -2. A-286501 showed equivalent potency in the inhibition of AK from several mammalian species and kinetic studies revealed that A-286501 was a reversible and competitive inhibitor with respect to ADO and non-competitive with respect to MgATP2-

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	328.17
Molecular Formula	C11H14BrN5O2
CAS No.	483341-15-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 10 mM
	Water: N/A
	Ethanol: N/A
Synonyms	A-286501; A 286501; A286501

Protocol	In Vitro	In vitro activity: Kinase Assay: Cell Assay:

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

Structures of the AK inhibitors. Pain. 2002 Mar;96(1-2):107-18.

Effects of AK inhibitors to attenuate thermal hyperalgesia (filled circles, n=6 per dose group), locomotor activity (open squares, n=6 per dose group) and rotorod performance. Pain. 2002 Mar;96(1-2):107-18.

Effects of ADO receptor agonists to attenuate thermal hyperalgesia (filled circles, n=6 per dose group), locomotor activity (open squares, n=6 per dose group) and rotorod performance. Pain. 2002 Mar;96(1-2):107-18.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	3.0472 mL	15.2360 mL	30.4720 mL	60.9440 mL
5mM	0.6094 mL	3.0472 mL	6.0944 mL	12.1888 mL
10mM	0.3047 mL	1.5236 mL	3.0472 mL	6.0944 mL
20mM	0.1524 mL	0.7618 mL	1.5236 mL	3.0472 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.