JD5037
目录号 : GC13660
JD5037 是一种有效的 CB1R 拮抗剂，IC50 为 1.5 nM。
Cas No.:1392116-14-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice: JD-5037 is formulated in vehicle (V; 1% Tween80, 4% DMSO, 95% Saline). Obese mice are treated chronically (28 d) with vehicle (V; 1% Tween80, 4% DMSO, 95% Saline), JD5037, or SLV319 at a dose of 3 mg/kg, i.p. Body weight and food intake are monitored daily. Mice are euthanized by cervical dislocation under anesthesia; the brain, hypothalamus, liver, and combined fat pads are removed, weighed, and snap-frozen, and trunk blood is collected for determining the endocrine and biochemical parameters[2]. |
References: [1]. Chorvat RJ. Peripherally restricted CB1 receptor blockers. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60. | |
Ki: 0.35 nM
JD5037 is an inverse agonist at CB1 receptors.
Endocannabinoids, lipid mediators, can elicit a broad range of effects through G protein-coupled CB1 and CB2 receptors. Activation of CB1R can promote food intake, increase lipogenesis in adipose tissue and liver, and cause insulin resistance and dyslipidemia, suggesting that the endocannabinoid/CB1R system is involved in obesity and metabolic complications.
In vitro: Previous study showed that JD5037 had high CB1R binding affinity and >700-fold CB1/CB2 selectivity when compared with SLV319. In addition, it was found that both SLV319 and JD5037 were CB1R inverse agonists, verified by GTPgS binding. Moreover, CB1R specificity of JD5037 was further confirmed as a potency ratio of >1,000 relative to a panel of 70 transporters, receptors, and ion channels [1].
In vivo: In mice with diet-induced obesity, the peripherally restricted JD5037 was found to be equieffective with its brain-penetrant parent compound in reducing appetite, body weight, hepatic steatosis, as well as insulin resistance, even though it did not occupy central CB1R or induce related behaviors. Moreover, appetite and weight reduction caused by JD5037 were mediated by resensitizing diet-induced obesity mice to endogenous leptin via reversing the hyperleptinemia by decreasing leptin expression and secretion by adipocytes and increasing leptin clearance through the kidney [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] J. Tam, R. Cinar, J. Liu, et al. Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metabolism 16, 167-179 (2012).
| Cas No. | 1392116-14-1 | SDF | |
| 化学名 | (2S)-2-[[[(4S)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[(4-chlorophenyl)sulfonyl]amino]methylene]amino]-3-methyl-butanamide | ||
| Canonical SMILES | ClC(C=C1)=CC=C1C2=NN(/C(N[C@@H](C(C)C)C(N)=O)=N/S(C3=CC=C(Cl)C=C3)(=O)=O)C[C@@H]2C4=CC=CC=C4 | ||
| 分子式 | C27H27Cl2N5O3S | 分子量 | 572.5 |
| 溶解度 | Soluble in DMSO | 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 | 1.7467 mL | 8.7336 mL | 17.4672 mL |
| 5 mM | 0.3493 mL | 1.7467 mL | 3.4934 mL |
| 10 mM | 0.1747 mL | 0.8734 mL | 1.7467 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。