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Description
INCB3284 is a potent, selective, and orally bioavailable hCCR2 Antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates. In human clinical trials, INCB3284 exhibited a pharmacokinetic profile suitable for once-a-day dosing (T 1/2 = 15 h). 
Chemical Structure
 
Chemical Name
N-(2-(((R)-1-((1r,4R)-4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl)pyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide dimethanesulfonate 
SMILES Code
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 
Theoretical Analysis
XingMo Cat#:XM391 
Product Name:INCB3284 mesylate 
Synonyms:INCB3284; INCB 3284; INCB-3284; INCB3284 mesylate; INCB3284 dimesylate. 
CAS#:887401-93-6 (mesylate); 887401-92-5 (free base). 
Chemical Formula:C28H39F3N4O10S2 
Molecular Weight:712.7532 
Technical Data

Appearance: solid powder             

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years)

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4 ℃ for short term (days to weeks), or -20 ℃ for long term (months).

 



WARNING: This product is for research use only, not for human or veterinary use

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