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INCB 3284 dimesylate

Cat. No. 4306 3 Citations Submit a Review Datasheet / COA / SDS
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Cat.No. 4306 - INCB 3284 dimesylate | C26H31F3N4O4.2CH4O3S | CAS No. 887401-93-6
Description: Selective CCR2 antagonist
Chemical Name: N-[2-[[(3R)-1-[trans-4-Hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-benzamide dimethanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective hCCR2 antagonist. Exhibits potent antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity (IC50 values are 3.7 and 4.7 nM respectively). Also displays weak hERG activity; inhibits the hERG potassium current (IC50 = 84μM). Orally bioavailable.

Technical Data

M. Wt 712.76
Formula C26H31F3N4O4.2CH4O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 887401-93-6
PubChem ID 11679268
InChI Key PNPNUHKICDECDH-SEBNIYPMSA-N
Smiles O=C(NCC(N[C@@H]2CCN([C@H]3CC[C@](C4=CC=C(OC)N=C4)(O)CC3)C2)=O)C1=CC(C(F)(F)F)=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 71.28 100
DMSO 71.28 100

Preparing Stock Solutions

The following data is based on the product molecular weight 712.76. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.4 mL 7.01 mL 14.03 mL
5 mM 0.28 mL 1.4 mL 2.81 mL
10 mM 0.14 mL 0.7 mL 1.4 mL
50 mM 0.03 mL 0.14 mL 0.28 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Xue et al (2011) Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist. ACS.Med.Chem.Lett. 2 450

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Keywords: INCB 3284 dimesylate, INCB 3284 dimesylate supplier, INCB3284, CCR2, antagonist, antagonists, hCCR2, human, chemokine, receptor, receptors, Chemokine, CC, Receptors, 4306, Tocris Bioscience

3 Citations for INCB 3284 dimesylate

Citations are publications that use Tocris products. Selected citations for INCB 3284 dimesylate include:

McMillin et al (2014) Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation 11 121 PMID: 25012628

Zhou et al (2015) Klotho gene deficiency causes salt-sensitive hypertension via monocyte chemotactic protein-1/CC chemokine receptor 2-mediated inflammation. Nat Commun 26 121 PMID: 24904083

Liu et al (2016) Cancer-associated fibroblasts promote hepatocellular carcinoma metastasis through chemokine-activated hedgehog and TGF-β pathways. Cancer Lett. 379 49 PMID: 27216982

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Literature in this Area

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