keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCX140 (CCX140-B) 是 CCR2 的拮抗剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 420 | 现货 | ||
5 mg | ¥ 597 | 现货 | ||
10 mg | ¥ 896 | 现货 | ||
25 mg | ¥ 1,344 | 现货 | ||
50 mg | ¥ 1,987 | 现货 | ||
100 mg | ¥ 2,981 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 697 | 现货 |
产品描述 | CCX140 (CCX140-B) (CCX140-B) is an antagonist of CCR2. |
靶点活性 | CCR5:7 μM (in Activated T lymphocytes), hCCR2:2.3 nM (kd)(in monocytes), CCR2:3 nM (in THP-1 cells) |
体外活性 | 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]. |
体内活性 | CCX140 also reduces urine output, glucose excretion, hepatic glycogen and triglyceride content and glucose 6-phosphatase levels[2]. Treatment of hCCR2 KI mice with CCX140 (CCX140-B) causes a dose-dependent reduction in the number of peritoneal leukocytes after thioglycollate challenge: CCX140 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 mice, the CCR2 antagonist completely blocks the recruitment of inflammatory macrophages to visceral adipose tissue. In DIO hCCR2 KI mice, treatment with 100 mg/kg CCX140 blocks the progressive increase in UAER and ACR. CCX140 maintains lower UAER and ACR values during the entire 8-wk dosing regimen[1]. The mice exhibit reduced hyperglycemia and insulinemia, improved insulin sensitivity, increased circulating adiponectin levels, decreased pancreatic islet size and increased islet number. |
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, CCX140-B |
分子量 | 495.86 |
分子式 | C20H13ClF3N5O3S |
CAS No. | 1100318-47-5 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 0.25 mg/mL (0.50 mM), sonification/heating is recommended.
DMSO: 100 mg/mL (201.67 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0167 mL | 10.0835 mL | 20.167 mL | 50.4175 mL |
5 mM | 0.4033 mL | 2.0167 mL | 4.0334 mL | 10.0835 mL | |
10 mM | 0.2017 mL | 1.0083 mL | 2.0167 mL | 5.0417 mL | |
20 mM | 0.1008 mL | 0.5042 mL | 1.0083 mL | 2.5209 mL | |
50 mM | 0.0403 mL | 0.2017 mL | 0.4033 mL | 1.0083 mL | |
100 mM | 0.0202 mL | 0.1008 mL | 0.2017 mL | 0.5042 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CCX140 1100318-47-5 Immunology/Inflammation Microbiology/Virology CCR CCX-140 CCX 140 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 CCX140-B Inhibitor inhibitor inhibit