J-2156 (TFA)

2387505-73-7

582.59

DMSO : 100 mg/mL (ultrasonic); H₂O : 100 mg/mL (ultrasonic)

GPCR/G Protein; Neuronal Signaling

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 has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
IC50 & Target: IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)
In Vitro: J-2156 TFA binds with nanomolar affinity to the human somatostatin receptor subtype 4 (hsst4: Ki=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (hsst1: Ki=0.5 uM; hsst2: Ki>5 uM; hsst3: Ki=1.4 uM; hsst5: Ki=0.54 uM) in Chinese hamster ovary (CHO) cells.
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.