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JD-5037

Names

[ CAS No. ]:
1392116-14-1

[ Name ]:
JD-5037

[Synonym ]:
(E)-N-([(4S)-3-(4-Chlorophenyl)-4-phenyl-4,5-dihydro-1H-pyrazol-1-yl]{[(4-chlorophenyl)sulfonyl]amino}methylene)-L-valinamide
JD5037
Butanamide, 2-[[(E)-[(4S)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[(4-chlorophenyl)sulfonyl]imino]methyl]amino]-3-methyl-, (2S)-
JD-5037

Biological Activity

[Description]:

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor
Research Areas >> Metabolic Disease

[Target]

IC50: 1.5 nM (CB1R)[1]


[In Vivo]

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[2]. 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].

[Animal admin]

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.

[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.

[3]. Mukhopadhyay B, et al. Cannabinoid receptor 1 promotes hepatocellular carcinoma initiation and progression through multiple mechanisms. Hepatology. 2015 May;61(5):1615-26.


[Related Small Molecules]

WIN 55212-2 mesylate | AM251 | Taranabant | SR144528 | Bay 59-3074 | Org 27569 | Otenabant | GW842166X | A-836339 | BML-190 | (±)-SLV319 | Pregnenolone | Anandamide | 2-arachidonoylglycerol | AM1241

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
731.3±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H27Cl2N5O3S

[ Molecular Weight ]:
572.506

[ Flash Point ]:
396.1±35.7 °C

[ Exact Mass ]:
571.121155

[ LogP ]:
4.58

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.662

[ Storage condition ]:
2-8℃

Related Compounds