Structure
CCX140, inhibitor
CCX140
Purity
98.00%
Synonyms
CCX140; CCX140-B; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
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)
H2O: 0.25mg/mL (0.50mM) Need ultrasonic and warming
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C20H13ClF3N5O3S
SMILES
FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl
CAS Number
1100318-47-5
Target & IC50
hCCR2: ic50 2.3nM (kd) (in monocytes)
CCR2: ic50 3nM (in THP-1 cells)
CCR5: ic50 7uM (in Activated T lymphocytes)
CCR2: ic50 3nM (in THP-1 cells)
CCR5: ic50 7uM (in Activated T lymphocytes)
In Vitro
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].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for CCX140, inhibitor
CCX140 (CCX140-B) is an antagonist of CCR2.
Product Categories/Family for CCX140, inhibitor
References
Sullivan T, et al. CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97.
Sullivan T, et al. CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97.
Sullivan TJ, et al. Experimental evidence for the use of CCR2 antagonists in the treatment,of type 2 diabetes. Metabolism. 2013 Nov;62(11):1623-32.
Sullivan TJ, et al. Experimental evidence for the use of CCR2 antagonists in the treatment,of type 2 diabetes. Metabolism. 2013 Nov;62(11):1623-32.
Sullivan T, et al. CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97.
Sullivan TJ, et al. Experimental evidence for the use of CCR2 antagonists in the treatment,of type 2 diabetes. Metabolism. 2013 Nov;62(11):1623-32.
Sullivan TJ, et al. Experimental evidence for the use of CCR2 antagonists in the treatment,of type 2 diabetes. Metabolism. 2013 Nov;62(11):1623-32.
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Product Notes
The CCX140 (Catalog #AAA5754687) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "CCX140, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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