Cis-INCB3344

CAT: 0804-HY-77111-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-77111-01Size:5 mg
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Description
Cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
CAS Number
[1285539-85-6]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
CCR; Drug Isomer
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation; Others
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Endocrinology; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/cis-incb3344.html
Purity
95.10
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(NCC(N[C@H]1CN([C@@H]2CC[C@](C3=CC=C(OCO4)C4=C3)(O)CC2)C[C@@H]1OCC)=O)C5=CC=CC(C(F)(F)F)=C5
Molecular Formula
C29H34F3N3O6
Molecular Weight
577.59
Precautions
H302, H315, H319, H335
References & Citations
[1]Xue CB, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. Bioorg Med Chem Lett. 2010 Dec 15;20 (24) :7473-8|[2]Zhao W, et al. Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. Hum Vaccin Immunother. 2017 Dec 2;13 (12) :2872-2882.|[3]Aye-Mon A, et al. CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. Mol Pain. 2018 Jan-Dec;14:1744806917751322.|[4]Chan CT, et al. Reversal of vascular macrophage accumulation and hypertension by a CCR2 antagonist in deoxycorticosterone/salt-treated mice. Hypertension. 2012 Nov;60 (5) :1207-12.|[5]Brodmerkel CM, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344. J Immunol. 2005 Oct 15;175 (8) :5370-8.|[6]Cassini MF, et al. Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. J Am Soc Nephrol. 2018 Oct;29 (10) :2471-2481.|[7]Dansereau MA, et al. Spinal CCL2 pronociceptive action is no longer effective in CCR2 receptor antagonist-treated rats. J Neurochem. 2008 Jul;106 (2) :757-69.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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