INCB 3284 dimesylate

Pricing Availability Delivery Time Qty
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)
Literature

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Select a batch to recalculate based on the batch molecular weight:
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 products' biological activity.

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


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Keywords: INCB3284 CCR2 antagonist antagonists hCCR2 human chemokine receptor receptors Chemokine CC Receptors

3 Citations for INCB 3284 dimesylate

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

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

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


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