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AMG 487 CXCR antagonist

Name: AMG 487
Brand: Selleck Chemicals
SKU: S8682
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S8682

AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.

Chemical Structure

Molecular Weight: 603.59

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Quality Control

Batch: S868201 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.86%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.86

Related Targets	PD-1/PD-L1 STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor
Other CXCR Inhibitors	AZD5069 SB 225002 Reparixin (Repertaxin) WZ811 Navarixin (SCH-527123) LIT-927 SX-682 LY2510924 UNBS5162 Danirixin (GSK1325756)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (165.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.28mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.14mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	603.59	Formula	C₃₂H₂₈F₃N₅O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	473719-41-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCOC1=CC=C(C=C1)N2C(=O)C3=CC=CN=C3N=C2C(C)N(CC4=CC=CN=C4)C(=O)CC5=CC=C(OC(F)(F)F)C=C5

Mechanism of Action

Targets/IC₅₀/Ki	CXCR3-CXCL10 (Cell-free assay) 8.0 nM CXCR3-CXCL11 (Cell-free assay) 8.2 nM
In vitro	AMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping.
In vivo	AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA).
References	[1] https://pubmed.ncbi.nlm.nih.gov/17448658/ [2] https://pubmed.ncbi.nlm.nih.gov/32239302/ [3] https://pubmed.ncbi.nlm.nih.gov/31449849/

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