CCX140 |
Catalog No.GC31330
One-Click Copy Product Info
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Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1100318-47-5
Sample solution is provided at 25 µL, 10mM.
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CCX140 is a potent CCR2 antagonist.
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-B also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140-B inhibits the binding of 125I-CCL2 to monocytes with an IC50 value of 17 nM. CCX140-B has a Kd value of 2.3 nM toward hCCR2. CCX140-B also inhibits monocyte chemotaxis mediated by the other CCR2 ligands: CCL8/MCP-2, CCL7/MCP-3, and CCL13/MCP-4[1].
Treatment of hCCR2 KI mice with CCX140-B causes a dose-dependent reduction in the number of peritoneal leukocytes after thioglycollate challenge: CCX140-B strongly blocks leukocyte infiltration at 30 mg/kg, partially blocks leukocyte infiltration at 10 mg/kg, and fails to block leukocyte infiltration at 3 mg/kg. In DIO hCCR2 KI mice, treatment with 100 mg/kg CCX140-B blocks the progressive increase in UAER and ACR. CCX140-B maintains lower UAER and ACR values during the entire 8-wk dosing regimen[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. It also reduces urine output, glucose excretion, hepatic glycogen and triglyceride content and glucose 6-phosphatase levels[2].
[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.
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Animal experiment: |
Mice: CCX140 is formulated as a solution in 1% hydroxypropyl methylcellulose. Male uninephrectomized hCCR2 KI mice are rendered diabetic with the high-fat diet and dosed with 100 mg/kg CCX140, but for 8 wk of dosing. Eight-week-old male hCCR2 KI Lepr db/db mice are similarly dosed with 100 mg/kg CCX140 for 6 wk[1]. |
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References: [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. |
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| Cas No. | 1100318-47-5 | SDF | |
| Canonical SMILES | FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl | ||
| Formula | C20H13ClF3N5O3S | M.Wt | 495.86 |
| Solubility | DMSO: ≥ 100 mg/mL (201.67 mM); Water: 0.25 mg/mL (0.50 mM and warming) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0167 mL | 10.0835 mL | 20.167 mL |
| 5 mM | 403.3 μL | 2.0167 mL | 4.0334 mL |
| 10 mM | 201.7 μL | 1.0083 mL | 2.0167 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)