| CAS NO: | 1392116-14-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 572.51 |
|---|---|
| Formula | C27H27Cl2N5O3S |
| CAS No. | 1392116-14-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mM |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | CC(C)[C@@H](C(N)=O)/N=C(N1N=C(C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC=C3)C1)/NS(=O)(C4=CC=C(Cl)C=C4)=O |
| Synonyms | JD-5037; JD 5037; JD5037; Chemical Name: (S)-2-(((E)-((S)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1H-pyrazol-1-yl)((4-chlorophenyl)sulfonamido)methylene)amino)-3-methylbutanamide Exact Mass: 571.1212 |
| In Vitro | In vitro activity: JD5037 is an inverse agonist of peripherally restricted (PR) cannabinoid 1 (CB1) receptors with Ki of 0.35 nM. Antagonists (inverse agonists) of the cannabinoid-1 (CB1) receptor showed promise as new therapies for controlling obesity and related metabolic function/liver disease. These agents, representing diverse chemical series, shared the property of brain penetration due to the initial belief that therapeutic benefit was mainly based on brain receptor interaction. JD5037 displays>700-fold selectivity for CB1 over CB2,>1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels, and low blood-brain barrier penetrance.JD5037 is orally bioavailable and reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obese mice. Kinase Assay: JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM. |
|---|---|
| In Vivo | 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. JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia, and reduces the HFD-induced hepatic injury and steatosis in obese Magel2-null mice |
| Animal model | Obesity mice |
| Formulation & Dosage | JD-5037 is formulated in vehicle (V; 1% Tween80, 4% DMSO, 95% Saline); 3 mg/kg, i.p. |
| References | Bioorg Med Chem Lett. 2013 Sep 1;23(17):4751-60 |
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