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Purity: ≥98%
JD5037 is a novel and potent inverse agonist of peripherally restricted (PR) cannabinoid 1 (CB1) receptors with Ki of 0.35 nM. The cannabinoid-1 (CB1) receptor agonists, also known as inverse agonists, have shown promise as novel treatments for obesity and associated metabolic disorders, including liver disease. Because it was originally thought that brain receptor interaction was primarily responsible for therapeutic benefit, these agents, representing different chemical series, shared the property of brain penetration. JD5037 has low blood-brain barrier penetration and >700-fold selectivity for CB1 over CB2 and >1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels. Orally bioavailable JD5037 decreases food intake, weight, and abnormalities related to hormones and metabolism in diet-induced obese mice.
| Targets |
Bcl-1 ( IC50 = 1.5 nM )
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| ln Vitro |
JD5037 is an inverse agonist with a Ki of 0.35 nM for peripherally restricted (PR) cannabinoid 1 (CB1) receptors. Inverse agonists, or antagonists, of the cannabinoid-1 (CB1) receptor have shown promise as novel treatments for obesity and associated metabolic disorders, including liver disease. Due to the early assumption that therapeutic benefit was primarily based on brain receptor interaction, these agents, representing different chemical series, shared the property of brain penetration. JD5037 exhibits low blood-brain barrier penetration and >700-fold selectivity for CB1 over CB2 as well as >1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels. Orally bioavailable JD5037 decreases food intake, body weight, and abnormalities related to hormones and metabolism in diet-induced obese mice.
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| ln Vivo |
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| Enzyme Assay |
JD-5037 is a new CB1R antagonist with an IC50 of 1.5 nM that is peripherally restricted.
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| Animal Protocol |
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| References |
| Molecular Formula |
C27H27CL2N5O3S
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| Molecular Weight |
572.505
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| Exact Mass |
571.12
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| Elemental Analysis |
C, 56.65; H, 4.75; Cl, 12.38; N, 12.23; O, 8.38; S, 5.60
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| CAS # |
1392116-14-1
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| Related CAS # |
1392116-14-1
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| Appearance |
Solid powder
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| SMILES |
CC(C)[C@@H](C(=O)N)N=C(NS(=O)(=O)C1=CC=C(C=C1)Cl)N2C[C@@H](C(=N2)C3=CC=C(C=C3)Cl)C4=CC=CC=C4
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| InChi Key |
GTCSIQFTNPTSLO-RPWUZVMVSA-N
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| InChi Code |
InChI=1S/C27H27Cl2N5O3S/c1-17(2)24(26(30)35)31-27(33-38(36,37)22-14-12-21(29)13-15-22)34-16-23(18-6-4-3-5-7-18)25(32-34)19-8-10-20(28)11-9-19/h3-15,17,23-24H,16H2,1-2H3,(H2,30,35)(H,31,33)/t23-,24+/m1/s1
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| Chemical Name |
(2S)-2-[[[(4S)-5-(4-chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-[(4-chlorophenyl)sulfonylamino]methylidene]amino]-3-methylbutanamide
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| Synonyms |
JD-5037; JD 5037; JD5037
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100~250 mg/mL ( 174.7~436.7 mM）
Water: Insoluble Ethanol: < 2 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7467 mL | 8.7335 mL | 17.4669 mL | |
| 5 mM | 0.3493 mL | 1.7467 mL | 3.4934 mL | |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7467 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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