INCB 3284 dimesylate

Modify Date: 2024-01-13 12:04:16

INCB 3284 dimesylate Structure
INCB 3284 dimesylate structure
 Common Name INCB 3284 dimesylate
CAS Number 887401-93-6 Molecular Weight 712.755
Density N/A Boiling Point N/A
Molecular Formula C28H39F3N4O10S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of INCB 3284 dimesylate


INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.

 Names

Name N-[2-[[(3R)-1-[4-hydroxy-4-(6-methoxypyridin-3-yl)cyclohexyl]pyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide,methanesulfonic acid
Synonym More Synonyms

 INCB 3284 dimesylate Biological Activity

Description INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.
Related Catalog
Target

MCP-1-hCCR2:3.7 nM (IC50)

In Vitro INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively[1].
In Vivo INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane[2].
Animal Admin Mice[2] Male C57Bl/6 mice (20 to 25 g) are given free access to water and rodent chow and are housed in constant temperature, humidity, and 12 h light-dark cycling. Acute liver failure is induced via a single intraperitoneal (ip) injection of 100 mg/kg of azoxymethane (AOM). In parallel, systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1 mg/kg/day ip) or C021 (1 mg/kg/day ip) for 3 days prior to injection of AOM. Following injection, mice are placed on heating pads adjusted to 37°C and monitored frequently for signs of neurological decline. To reduce the impacts of hypoglycemia and dehydration, cage floors are supplied with hydrogel and rodent chow and after 12 h, and every subsequent 4 h, mice are injected subcutaneously with 5% dextrose in 250 μL of saline. If mice undergo a 20% or greater weight loss they are removed from the study[2].
References

[1]. Xue CB, et al. Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4.

[2]. McMillin M, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121.

 Chemical & Physical Properties

Molecular Formula C28H39F3N4O10S2
Molecular Weight 712.755
Exact Mass 712.205994
PSA 229.29000
LogP 4.74900
Storage condition 2-8℃

 Synonyms

cc-408
N-[2-({(3R)-1-[cis-4-Hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl}amino)-2-oxoethyl]-3-(trifluoromethyl)benzamide methanesulfonate (1:2)
INCB 3284 dimesylate||INCB3284 dimesylate
INCB3284 dimesylate
Benzamide, N-[2-[[(3R)-1-[cis-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, methanesulfonate (1:2) (salt)
CS-0958
INCB 3284 (dimesylate)
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