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MK-0812 Succinate
🥰Excellent
Catalog No. T16091Cas No. 851916-42-2
MK-0812 Succinate is an effective and selective CCR2 antagonist.
MK-0812 Succinate
🥰Excellent
Purity: 98.62%
Catalog No. T16091Cas No. 851916-42-2
MK-0812 Succinate is an effective and selective CCR2 antagonist.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $59 | In Stock | |
| 5 mg | $147 | In Stock | |
| 10 mg | $277 | In Stock | |
| 25 mg | $562 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $189 | In Stock |
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Purity:98.62%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | MK-0812 Succinate is an effective and selective CCR2 antagonist. It also has a high affinity at CCR2. |
| 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 |
| 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 |
| Relative Density. | 1.31g/cm3 |
Storage & Solubility Information
| 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), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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