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MK-0812 Succinate

Catalog No. T16091 CAS 851916-42-2

MK-0812 Succinate is an effective and selective CCR2 antagonist.

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MK-0812 Succinate, CAS 851916-42-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 59.00
2 mg	In stock	$ 85.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 277.00
25 mg	In stock	$ 562.00
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 189.00

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Purity: 98.62%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MK-0812 Succinate is an effective and selective CCR2 antagonist.
Targets&IC50	MCP-1:4.5 nM
In vitro	MK-0812 not only fully blocks the shape change response to exogenous MCP-1 but also causes a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM. MK-0812 fully blocks all MCP-1 mediated response in a concentration-dependent manner (IC50: 3.2 nM). This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50: 4.5 nM) [2].
In vivo	MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in the blood. MK-0812 treatment induces a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2. MK-0812 (30 mg/kg, p.o.) decreases the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed [1][2].

Molecular Weight	587.63
Formula	C28H40F3N3O7
CAS No.	851916-42-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (47.65 mM)

References and Literature

1. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis.Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. 2. Wisniewski T, et al. Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.J Immunol Methods. 2010 Jan 31;352(1-2):101-10.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Chemokine Inhibitor Library Clinical Compound Library ReFRAME Related Library Immunology/Inflammation Compound Library Cytokine Inhibitor Library

Related Products

Related compounds with same targets

CCR1 antagonist 6 MK-0812 Cenicriviroc CCX140 5-Hydroxy-7,8-dimethoxyflavanone 3-(hydroxymethyl)cyclopentanone Pirfenidone CCR2-RA-[R]

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Keywords

MK-0812 Succinate 851916-42-2 Immunology/Inflammation Microbiology/Virology Others CCR CC chemokine receptor MK 0812 Inhibitor MK0812 Succinate MK 0812 Succinate MK0812 MK-0812 inhibit inhibitor

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