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J-2156

Names

[ CAS No. ]:
848647-56-3

[ Name ]:
J-2156

Biological Activity

[Description]:

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor
Research Areas >> Others

[Target]

IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)[1]


[In Vivo]

J-2156 (1-10 mg/kg; i.p.; for 3 hours) of single bolus doses has anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats[1]. Animal Model: BCIBP-rats[1] Dosage: 1, 3, 10 mg/kg Administration: I.p.; for 3 hours Result: Had anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats.

[References]

[1]. Shenoy PA, et al. The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain. Front Pharmacol. 2018 May 15;9:495.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28N4O4S

[ Molecular Weight ]:
468.57


Related Compounds