4-Quinolone-3-Carboxamide Furan CB2 Agonist (Synonyms:CB2 receptor agonist 2)
目录号 : KCM11011 CAS No. : 1314230-75-5 纯度 : ≥98%
Agonists of the peripheral cannabinoid (CB) receptor CB may have antinociceptive and anti-inflammatory effects, as well as prevent osteoporosis. 4-Quinolone-3-carboxamide Furan CB Agonist is a high-affinity ligand of CB (K = 8.5 nM) with little affinity for CB (K >10,000 nM). This compound demonstrates antinociceptive efficacy in the mouse formalin test at 1 mg/kg, an action which is blocked by a CB-selective antagonist, AM630 .
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1mg
¥1102.00
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5mg
¥4977.00
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10mg
¥8820.00
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25mg
¥19309.00
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生物活性

4-Quinolone-3-Carboxamide Furan CB2 Agonist is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. 4-Quinolone-3-Carboxamide Furan CB2 Agonist has high affinity and selectivity for CB2.

体外研究

4-Quinolone-3-Carboxamide Furan CB2 Agonist (1 μM; 72 hours) has very low or no cytotoxicity to Hep-G2 cells.

 

Cell Proliferation Assay

Cell Line: Hep-G2 (Human hepatoblastoma) cells
Concentration: 1  μM
Incubation Time: 72 hours
Result: Exhibited very low or no cytotoxicity to Hep-G2 cells.
体内研究

4-Quinolone-3-Carboxamide Furan CB2 Agonist (1 and 3 mg/kg; 1 hour) is very potent (with maximal effect being reached already at the 1 mg/kg dose) and has antihyperalgesic effects, efficacious also on the first phase of the nocifensive response and strongly reduced by AM630 (CB2-selective antagonist/inverse agonist) .

 

Animal Model: Formalin injection induces a biphasic stereotypical nocifensive behavior in mice
Dosage: Formalin (1.25% in saline, 30 μL), 1 and 3 mg/kg CB2 receptor agonist 2, 1 mg/kg AM630, monitor every 5 minutes for 1 hour
Administration: Injection in the dorsal surface of one side of the hindpaw (Formalin), i.p. (CB2 receptor agonist, AM630)
Result:
Elicited antihyperalgesic effects and potent (with maximal effect being reached already at the 1 mg/kg dose) and efficacious, strongly reduced by AM630.
 
分子式
C30H36N2O4
分子量
488.62
CAS号
1314230-75-5
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

Ethanol : 30 mg/mL (61.40 mM; Need ultrasonic and warming)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.0466 mL 10.2329 mL 20.4658 mL
5 mM 0.4093 mL 2.0466 mL 4.0932 mL
10 mM 0.2047 mL 1.0233 mL 2.0466 mL
*

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, 6 months; -20°C, 1 month。-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。

科研文献

CB2

8.5 nM (Ki)

暂无相关参考文献
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动物实验计算换算器
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)
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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 ddH2O,混匀澄清。

配置后的溶液总体积

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。