Product Details
Product Name:
MK-0812 Succinate |
CAS No.:
851916-42-2 |
Purity:
98.62% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | MK-0812 Succinate |
Description | MK-0812 Succinate is an effective and selective CCR2 antagonist. |
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 28 mg/mL (47.65 mM)
|
Keywords | MK-0812 Succinate | CC chemokine receptor | MK 0812 | Inhibitor | MK0812 Succinate | MK 0812 Succinate | CCR | MK0812 | MK-0812 | inhibit |
Inhibitors Related | AZD2098 | MLN-3897 TFA | Artemotil | CCR2 antagonist 5 | INCB-9471 | CCR3 antagonist 1 | Maraviroc | BMS-817399 | PF-4136309 | Pirfenidone | Vercirnon | CCR6 antagonist 1 |
Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Chemokine Inhibitor Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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