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J 2156

Names

[ CAS No. ]:
2387505-73-7

[ Name ]:
J 2156

Biological Activity

[Description]:

J-2156 TFA 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. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor
Research Areas >> Neurological Disease

[Target]

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


[In Vitro]

J-2156 TFA binds with nanomolar affinity to the human somatostatin receptor subtype 4 (h sst4: Ki=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (h sst1: Ki=1.2 nM; h sst2: Ki>5000 nM; h sst3: Ki=1400 nM; h sst5: Ki=540 nM) in Chinese hamster ovary (CHO) cells[2].

[In Vivo]

J-2156 TFA (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: Breast cancer-induced bone pain (BCIBP)-rats[1] Dosage: 1, 3, 10 mg/kg Administration: IP; 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.

[2]. Mia Engström, et al. Superagonism at the Human Somatostatin Receptor Subtype 4. J Pharmacol Exp Ther. 2005 Jan;312(1):332-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H29F3N4O6S

[ Molecular Weight ]:
582.59

Related Compounds