JD5037

  • CAT Number: I007410
  • CAS Number: 1392116-14-1
  • Molecular Formula: C27H27Cl2N5O3S
  • Molecular Weight: 572.5
  • Purity: ≥95%
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JD5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker. JD5037 is an antiobesity drug candidate which acts as a peripherally-restricted cannabinoid inverse agonist at CB1 receptors. It is very selective for the CB1 subtype, with a Ki of 0.35nM, >700-fold higher affinity than it has for CB2 receptors. In animal studies, JD5037 does not readily cross the blood brain barrier and thus is not expected to produce the psychiatric side effects in humans which led to the withdrawal of rimonabant from the market. Its antiobesity effects are believed to be mediated by blockade of peripheral CB1 receptors, resulting in decreased leptin expression and secretion and increased leptin clearance by the kidneys.

Catalog Number I007410
CAS Number 1392116-14-1
Synonyms

JD5037; JD-5037; JD 5037.;(S)-2-(((E)-((S)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1H-pyrazol-1-yl)((4-chlorophenyl)sulfonamido)methylene)amino)-3-methylbutanamide

Molecular Formula

C27H27Cl2N5O3S

Purity 95%
Target Cannabinoid Receptor
Solubility Soluble in DMSO
Storage Store at -20°C
InChI 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
InChIKey GTCSIQFTNPTSLO-RPWUZVMVSA-N
SMILES ClC(C=C1)=CC=C1C2=NN(/C(N[C@@H](C(C)C)C(N)=O)=N/S(C3=CC=C(Cl)C=C3)(=O)=O)C[C@@H]2C4=CC=CC=C4
Reference

</br>1:Cinar R, Godlewski G, Liu J, Tam J, Jourdan T, Mukhopadhyay B, Harvey-White J, Kunos G. Hepatic cannabinoid-1 receptors mediate diet-induced insulin resistance by increasing de novo synthesis of long-chain ceramides. Hepatology. 2014 Jan;59(1):143-53. doi: 10.1002/hep.26606. PubMed PMID: 23832510; PubMed Central PMCID: PMC3839256.

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