JD-5037 Property

Boiling point:

721.6±70.0 °C(Predicted)

Density 

1.40±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥143.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

pka

10.63±0.60(Predicted)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

JD-5037 Chemical Properties,Usage,Production

Uses

JD 5037 is an anti-obesity drug candidate which acts as a peripherally-cannabinoid inverse agonist. Acts on the CB1 receptors.

Biological Activity

ki: 0.35 nmjd5037 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].

References

[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).