An antagonist of the MCP-1 receptor CCR2
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INCB 3284 (dimesylate)

Item No. 11963

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[(3R)-1-[trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-benzamide, dimethanesulfonate
CAS Number
887401-93-6
Molecular Formula
C26H31F3N4O4 • 2CH3SO3H
Formula Weight
712.8
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 11 mg/mlDMSO: 12 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
220, 274 nm
SMILES
O[C@]1(C2=CN=C(OC)C=C2)CC[C@@H](N3C[C@H](NC(CNC(C4=CC(C(F)(F)F)=CC=C4)=O)=O)CC3)CC1.CS(=O)(O)=O.CS(=O)(O)=O
InChi Code
InChI=1S/C26H31F3N4O4.2CH4O3S/c1-37-23-6-5-19(14-30-23)25(36)10-7-21(8-11-25)33-12-9-20(16-33)32-22(34)15-31-24(35)17-3-2-4-18(13-17)26(27,28)29;2*1-5(2,3)4/h2-6,13-14,20-21,36H,7-12,15-16H2,1H3,(H,31,35)(H,32,34);2*1H3,(H,2,3,4)/t20-,21-,25-;;/m1../
InChi Key
PNPNUHKICDECDH-FBLZNNLISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $40

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    5 mg

    $104

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    10 mg

    $128

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    50 mg

    $589

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    Cayman Chemical
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    Product Description

    INCB 3284 is a potent, selective, and orally bioavailable antagonist of monocyte chemotactic protein-1 binding to CCR2 (IC50 = 3.7 nM).1 For comparison, it has no significant inhibitor action at over 50 ion channels, transporters, GPCRs, and other chemokine receptors when tested at a concentration of 1 μM.1 INCB 3284 inhibits chemotaxis in vitro (IC50 = 4.7 nM) and displays acceptable oral bioavailability in mice, rats, dogs, monkeys, and chimpanzees.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xue, C.B., Feng, H., Cao, G., et al. Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist. ACS Med. Chem. Lett. 2, 450-454 (2011).