MK-0812 Succinate

SKU: orb1308034

Description

MK-0812 Succinate

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 851916-42-2
• MW: 587.63
• Purity: 99.93%
• Formula: C₂₈H₄₀F₃N₃O₇
• SMILES: OC(=O)CCC(O)=O.CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2ncc(cc2C1)C(F)(F)F
• Target: CCR
• Solubility: DMSO:28 mg/mL (47.65 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.4 mM)

Bioactivity

• Target IC50:
  MCP-1:4.5 nM
• 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 .
• 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) .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MCP-1, inhibit, MK 0812, MK 0812 Succinate, MK0812, MK-0812, MK0812 Succinate, MK-0812 Succinate, CC chemokine receptor, CCR2, CCR

Compound Identifiers

PubChem CID

11180807