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Submit ReviewINCB 3284 dimesylate
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)
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 the degree 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
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:
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
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
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
Do you know of a great paper that uses INCB 3284 dimesylate from Tocris? Please let us know.
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