A CCR2 antagonist
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MK-0812

Item No. 21803

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,5-anhydro-2,3-dideoxy-3-[[(1R,3S)- 3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]amino]-4-O-methyl-D-erythro-pentitol
CAS Number
624733-88-6
Molecular Formula
C24H34F3N3O3
Formula Weight
469.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:20): 0.04 mg/mlDMSO: 1 mg/mlEthanol: 10 mg/ml
λmax
267 nm
SMILES
O=C([C@@]1(C(C)C)CC[C@@H](N[C@]2([H])[C@H](OC)COCC2)C1)N(C3)CCC4=C3C=C(C(F)(F)F)C=N4
InChi Code
InChI=1S/C24H34F3N3O3/c1-15(2)23(7-4-18(11-23)29-20-6-9-33-14-21(20)32-3)22(31)30-8-5-19-16(13-30)10-17(12-28-19)24(25,26)27/h10,12,15,18,20-21,29H,4-9,11,13-14H2,1-3H3/t18-,20+,21-,23+/m1/s1
InChi Key
MTMDXAIUENDNDL-RJSMDTJLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $81

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    10 mg

    $593

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    Cayman Chemical
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    Product Description

    MK-0812 is an antagonist of chemokine (C-C) motif receptor 2 (CCR2; IC50 = 5 nM for the human receptor).1 It inhibits mammosphere formation of BT-549 breast cancer cells, an effect that is enhanced by the β-catenin inhibitor PNU 74654 (Item No. 16349).2 MK-0812 (0.03, 0.1, and 0.3 mg/kg) increases chemokine (C-C) motif ligand 2 (CCL2) levels and decreases CD11b+ monocytes in mouse blood.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Abagyan, R., Christopoulos, A., de Esch, I.J.P., et al. Chemokines. Chemokines and their receptors in drug discovery. 1-248 (2015).

    2. Zhang, F., Li, P., Liu, S., et al. β-Catenin-CCL2 feedback loop mediates crosstalk between cancer cells and macrophages that regulates breast cancer stem cells. Oncogene 40(39), 5854-5865 (2021).

    3. Min, S.-H., Wang, Y., Gonsiorek, W., et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem. Biophys. Res. Commun. 391(1), 1080-1086 (2010).