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CCX140

Catalog No. T14909 CAS 1100318-47-5

Synonyms: CCX140-B

CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.

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CCX140, CAS 1100318-47-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 50.00
5 mg	In stock	$ 62.00
10 mg	In stock	$ 92.00
25 mg	In stock	$ 138.00
50 mg	In stock	$ 205.00
100 mg	In stock	$ 308.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.95%

Purity: 97.58%

Biological Description

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Storage & Solubility Information

Description	CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2.
Targets&IC50	CCR5:7 μM (in Activated T lymphocytes), CCR2 (human):2.3 nM (kd)(in monocytes), CCR2:3 nM (in THP-1 cells)
In vitro	CCX140 inhibits the binding of 125I-CCL2 to monocytes with an IC50 value of 17 nM and it also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140 (CCX140-B) potently inhibits CCL2-induced chemotaxis of purified human blood monocytes with IC50 values of 8 nM in buffer and 200 nM in the presence of 100% human serum. CCX140 has a Kd value of 2.3 nM toward hCCR2. CCX140 also inhibits monocyte chemotaxis mediated by the other CCR2 ligands: CCL8/MCP-2, CCL7/MCP-3, and CCL13/MCP-4[1].
In vivo	CCX140 effectively moderates various metabolic and immunological parameters. It decreases urine and glucose excretion, lowers hepatic glycogen and triglyceride contents, and reduces glucose 6-phosphatase levels. In hCCR2 KI mice, CCX140-B dosage exhibits a significant, dose-dependent capability to mitigate peritoneal leukocyte count following thioglycollate induction, displaying robust leukocyte infiltration inhibition at 30 mg/kg, partial inhibition at 10 mg/kg, and no effect at 3 mg/kg. Additionally, in diet-induced obese (DIO) mice, CCX140 acts as a CCR2 antagonist, fully preventing inflammatory macrophage recruitment to visceral adipose tissue. For DIO hCCR2 KI mice treated with 100 mg/kg of CCX140, there's an evident halt in the escalating urine albumin excretion rate (UAER) and albumin to creatinine ratio (ACR), with sustained lower levels throughout an 8-week dosage period. The treated mice also show reduced hyperglycemia and insulin levels, enhanced insulin sensitivity, escalated circulating adiponectin levels, diminished pancreatic islet size, and an increase in islet number, demonstrating CCX140's comprehensive therapeutic potential.

Synonyms	CCX140-B
Molecular Weight	495.86
Formula	C20H13ClF3N5O3S
CAS No.	1100318-47-5

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 0.25 mg/mL (0.50 mM), Sonication and heating are recommended.

DMSO: 100 mg/mL (201.67 mM)

References and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library Immunology/Inflammation Compound Library Covalent Inhibitor Library Cytokine Inhibitor Library Bioactive Compound Library Immuno-Oncology Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Chemokine Inhibitor Library

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Keywords

CCX140 1100318-47-5 Immunology/Inflammation Microbiology/Virology CCR CCX-140 CCX 140 CCX140-B inhibitor inhibit

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