JD-5037
Based on 9 publication(s) in Google Scholar
JD-5037 is a potent CB1R antagonist with an IC50 of 1.5 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.38%
- CAS. Nr.: 1392116-14-1
- Formel: C27H27Cl2N5O3S
- Molecular Weight:572.51
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) JD-5037
More- Cell. 2025 Dec 24;188(26):7547-7570.e45 [Abstract]
- Nat Commun. 2022 Apr 4;13(1):1783. [Abstract]
- Diabetologia. 2024 Sep;67(9):1877-1896. [Abstract]
- J Am Soc Nephrol. 2017 Dec;28(12):3518-3532. [Abstract]
- Br J Pharmacol. 2020 Jan;177(1):110-127. [Abstract]
- Diabetes. 2020 Oct;69(10):2120-2132. [Abstract]
- Elife. 2020 Nov 19;9:e60771. [Abstract]
- Mol Cell Endocrinol. 2021 Jun 1:529:111267. [Abstract]
- Cannabis Cannabinoid Res. 2023 Aug;8(4):623-633. [Abstract]
Customer Validation & Images
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WB
Biologische Aktivität
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CB1 1.5 nM (IC50) |
JD5037 (3 mg/kg/day, p.o.) significantly reduces the size of tumors and abrogates the tumor in DEN-treated mice. JD5037 attenuates the AEA levels in HCC samples from mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1392116-14-1
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Appearance Solid
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Molecular Weight 572.51
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Formel C27H27Cl2N5O3S
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Color White to off-white
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SMILES
NC([C@H](C(C)C)/N=C(NS(=O)(C1=CC=C(Cl)C=C1)=O)\N2N=C(C3=CC=C(Cl)C=C3)[C@@H](C4=CC=CC=C4)C2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell
In vivo transcriptomic, functional, circuit-based, and translational analyses of enteric neurons. [Abstract]2025 Dec 24;188(26):7547-7570.e45 PMID: 41406962 -
Nat Commun
Opposite physiological and pathological mTORC1-mediated roles of the CB1 receptor in regulating renal tubular function. [Abstract]2022 Apr 4;13(1):1783. PMID: 35379807 -
Diabetologia
Pharmaceutical targeting of the cannabinoid type 1 receptor impacts the crosstalk between immune cells and islets to reduce insulitis in humans. [Abstract]2024 Sep;67(9):1877-1896. PMID: 38864887 -
J Am Soc Nephrol
2017 Dec;28(12):3518-3532. PMID: 28860163
JD-5037 purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2017 Dec;28(12):3518-3532. [Abstract]
The peripheral blockade of CB1R by JD5037 (3 mg/kg, administered orally) significantly normalizes the expression levels of pLKB1.
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Br J Pharmacol
Dual inhibition of cannabinoid CB1 receptor and inducible NOS attenuates obesity-induced chronic kidney disease. [Abstract]2020 Jan;177(1):110-127. PMID: 31454063 -
Diabetes
Simultaneous Inhibition of Peripheral CB1R and iNOS Mitigates Obesity-Related Dyslipidemia Through Distinct Mechanisms. [Abstract]2020 Oct;69(10):2120-2132. PMID: 32680936 -
Elife
CB1R regulates soluble leptin receptor levels via CHOP, contributing to hepatic leptin resistance. [Abstract]2020 Nov 19;9:e60771. PMID: 33210603 -
Mol Cell Endocrinol
2021 Jun 1:529:111267. PMID: 33839219 -
Cannabis Cannabinoid Res
2023 Aug;8(4):623-633. PMID: 35647939
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (174.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (4.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Chorvat RJ. Peripherally restricted CB1 receptor blockers. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60. [Content Brief]
[2]. Knani I, et al. Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome. Mol Metab. 2016 Oct 22;5(12):1187-1199. [Content Brief]
[3]. Mukhopadhyay B, et al. Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms. Hepatology. 2015 May;61(5):1615-26. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7467 mL | 8.7335 mL | 17.4669 mL | 43.6674 mL |
| 5 mM | 0.3493 mL | 1.7467 mL | 3.4934 mL | 8.7335 mL | |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7467 mL | 4.3667 mL | |
| 15 mM | 0.1164 mL | 0.5822 mL | 1.1645 mL | 2.9112 mL | |
| 20 mM | 0.0873 mL | 0.4367 mL | 0.8733 mL | 2.1834 mL | |
| 25 mM | 0.0699 mL | 0.3493 mL | 0.6987 mL | 1.7467 mL | |
| 30 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4556 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4367 mL | 1.0917 mL | |
| 50 mM | 0.0349 mL | 0.1747 mL | 0.3493 mL | 0.8733 mL | |
| 60 mM | 0.0291 mL | 0.1456 mL | 0.2911 mL | 0.7278 mL | |
| 80 mM | 0.0218 mL | 0.1092 mL | 0.2183 mL | 0.5458 mL | |
| 100 mM | 0.0175 mL | 0.0873 mL | 0.1747 mL | 0.4367 mL |
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