1262238-11-8 Usage
Description
INCB3344 is an antagonist of chemokine (C-C motif) receptor 2 (CCR2) with high selectivity and potency (IC50 = 10 nM in WEHI-274 murine monocytes). It effectively inhibits chemotaxis, ERK phosphorylation, and monocyte influx in various mouse models, demonstrating its potential in modulating immune responses and inflammation.
Uses
Used in Immunology and Inflammation Research:
INCB3344 is used as a selective antagonist for CCR2, a G protein-coupled receptor, to study its role in chemotaxis, immune cell migration, and inflammation. Its high selectivity over other receptors, such as CCR1 and CCR5, makes it a valuable tool for investigating the specific functions of CCR2 in various biological processes.
Used in Autoimmune Disease Treatment:
INCB3344 is used as a potential therapeutic agent for autoimmune diseases, such as experimental autoimmune encephalomyelitis (EAE), by reducing the expression of CCR2 mRNA, preventing macrophage infiltration, and decreasing disease incidence and severity.
Used in Inflammatory Conditions:
INCB3344 is used to alleviate inflammation in conditions like peritonitis and delayed-type hypersensitivity reactions, as demonstrated by its ability to reduce ear swelling and monocyte influx in mouse models.
Used in Arthritis Treatment:
INCB3344 is used as a potential treatment for adjuvant-induced arthritis in rats, as it has been shown to reduce disease severity.
Used in Polycystic Kidney Disease Management:
INCB3344 is used to reduce macrophage infiltration to the kidney and improve renal function in mouse models of polycystic kidney disease, suggesting its potential in managing this condition.
references
[1]. brodmerkel c m, huber r, covington m, et al. discovery and pharmacological characterization of a novel rodent-active ccr2 antagonist, incb3344[j]. the journal of immunology, 2005, 175(8): 5370-5378.
Check Digit Verification of cas no
The CAS Registry Mumber 1262238-11-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,6,2,2,3 and 8 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1262238-11:
(9*1)+(8*2)+(7*6)+(6*2)+(5*2)+(4*3)+(3*8)+(2*1)+(1*1)=128
128 % 10 = 8
So 1262238-11-8 is a valid CAS Registry Number.
1262238-11-8Relevant articles and documents
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2
Xue, Chu-Biao,Wang, Anlai,Meloni, David,Zhang, Ke,Kong, Ling,Feng, Hao,Glenn, Joseph,Huang, Taisheng,Zhang, Yingxin,Cao, Ganfeng,Anand, Rajan,Zheng, Changsheng,Xia, Michael,Han, Qi,Robinson,Storace, Lou,Shao, Lixin,Li, Mei,Brodmerkel, Carrie M.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
experimental part, p. 7473 - 7478 (2011/01/12)
Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led to the
