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CCX140

Cat. No. M8986
CCX140 Structure
Synonym:

CCX140-B

Size Price Availability Quantity
5mg USD 190 In stock
10mg USD 300 In stock
50mg USD 1080 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CCX140 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-B also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140-B has a Kd value of 2.3 nM toward hCCR2.

In vivo, CCX140-B(100 mg/kg) treatment in DIO hCCR2 KI mice blocks the progressive increase in UAER and ACR. CCX140-B maintains lower UAER and ACR values during the entire 8-wk dosing regimen.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 495.86
Formula C20H13ClF3N5O3S
CAS Number 1100318-47-5
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice.
Sullivan T, et al. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97. PMID: 23986513.

Experimental evidence for the use of CCR2 antagonists in the treatment of type 2 diabetes.
Sullivan TJ, et al. Metabolism. 2013 Nov;62(11):1623-32. PMID: 23953944.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCX140, CCX140-B supplier, CCR, inhibitors

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