| Bioactivity | 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. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2]. |
| Target | IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4) |
| Invitro | J-2156 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 (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: |
| Name | J-2156 |
| CAS | 848647-56-3 |
| Formula | C24H28N4O4S |
| Molar Mass | 468.57 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |