JD5037 |
Catalog No.GC13660
One-Click Copy Product Info
|
inverse agonist at CB1 receptors
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1392116-14-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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).
|
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. |
|
| Cas No. | 1392116-14-1 | SDF | |
| Chemical Name | (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 | ||
| Formula | C27H27Cl2N5O3S | M.Wt | 572.5 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7467 mL | 8.7336 mL | 17.4672 mL |
| 5 mM | 349.3 μL | 1.7467 mL | 3.4934 mL |
| 10 mM | 174.7 μL | 873.4 μL | 1.7467 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)