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]} .

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

J-2156 TFA binds with nanomolar affinity to the human somatostatin receptor subtype 4 (hsst4: K_i=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (hsst1: K_i=1.2 nM; hsst2: K_i>5000 nM; hsst3: K_i=1400 nM; hsst5: K_i=540 nM) in Chinese hamster ovary (CHO) cells^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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2387505-73-7

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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 Engstr?m, et al. Superagonism at the Human Somatostatin Receptor Subtype 4. J Pharmacol Exp Ther. 2005 Jan;312(1):332-8.