CCX140 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

495.86

DMSO: 100mg/mL (201.67mM)
H2O: 0.25mg/mL (0.50mM) Need ultrasonic and warming
(<1mg/ml refers to the product slightly soluble or insoluble)

C20H13ClF3N5O3S

FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl

1100318-47-5

hCCR2: ic50 2.3nM (kd) (in monocytes)
CCR2: ic50 3nM (in THP-1 cells)
CCR5: ic50 7uM (in Activated T lymphocytes)

In DIO hCCR2 KI mice, treatment with 100mg/kg CCX140 blocks the progressive increase in UAER and ACR. CCX140 maintains lower UAER and ACR values during the entire 8-wk dosing regimen. treatment of hCCR2 KI mice with CCX140 causes a dose-dependent reduction in the number of peritoneal leukocytes after thioglycollate challenge: CCX140 strongly blocks leukocyte infiltration at 30mg/kg, partially blocks leukocyte infiltration at 10mg/kg, and fails to block leukocyte infiltration at 3mg/kg [1]. In DIO mice, the CCR2 antagonist completely blocks the recruitment of inflammatory macrophages to visceral adipose tissue. The mice exhibit reduced hyperglycemia and insulinemia, improved insulin sensitivity, increased circulating adiponectin levels, decreased pancreatic islet size, and increased islet number. CCX140 also reduces glucose excretion, urine output, hepatic glycogen, and triglyceride content and glucose 6-phosphatase levels [2].

Immunology/Inflammation; CCR; Microbiology&virology