CCX140
(Synonyms: 3-三氟甲基-4-氯-N-[2-[7H-吡咯并[2,3-D]嘧啶-4-羰基]-5-甲基-3-吡啶基]苯磺酰胺) 目录号 : GC31330
CCX140是一种有效的CCR2拮抗剂。
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.
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]. |
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. | |
| Cas No. | 1100318-47-5 | SDF | |
| 别名 | 3-三氟甲基-4-氯-N-[2-[7H-吡咯并[2,3-D]嘧啶-4-羰基]-5-甲基-3-吡啶基]苯磺酰胺 | ||
| Canonical SMILES | FC(F)(F)C1=CC(S(=O)(NC2=CC(C)=CN=C2C(C3=NC=NC4=C3C=CN4)=O)=O)=CC=C1Cl | ||
| 分子式 | C20H13ClF3N5O3S | 分子量 | 495.86 |
| 溶解度 | DMSO: ≥ 100 mg/mL (201.67 mM); Water: 0.25 mg/mL (0.50 mM and warming) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0167 mL | 10.0835 mL | 20.167 mL |
| 5 mM | 0.4033 mL | 2.0167 mL | 4.0334 mL |
| 10 mM | 0.2017 mL | 1.0083 mL | 2.0167 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet