MK-0812 (Succinate)
MK-0812 (Succinate) Basic information
- Product Name:
- MK-0812 (Succinate)
- Synonyms:
-
- MK-0812 (Succinate)
- MK-0812 HCL
- MK 0812 SUCCINATE;MK0812 SUCCINATE
- CC chemokine receptor,MK 0812,Inhibitor,MK0812 Succinate,CCR,MK 0812 Succinate,MK0812,MK-0812,inhibit
- MK-0812 Succinate, 10 mM in DMSO
- CAS:
- 851916-42-2
- MF:
- C28H40F3N3O7
- MW:
- 587.64
- Mol File:
- 851916-42-2.mol
MK-0812 (Succinate) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 32 mg/mL (54.46 mM)
- form
- Solid
- color
- White to off-white
MK-0812 (Succinate) Usage And Synthesis
Description
MK0812 Succinate is a dual CCR2-CCR5 receptor antagonist.
Uses
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.
in vivo
MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2[1]. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[2].
IC 50
CCR2
References
[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. DOI:10.1016/j.bbrc.2009.12.025
[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. DOI:10.1016/j.jim.2009.10.010
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