产品
编 号:F618342
分子式:C26H29F3N4O6S
分子量:582.59
产品类型
结构图
CAS No: 2387505-73-7
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产品详情
生物活性:
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.
体内研究:
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.Animal Model:Breast cancer-induced bone pain (BCIBP)-rats
Dosage:1, 3, 10?mg/kg
Administration:IP; for 3 hours
Result:Had anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats.
体外研究:
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 μM; hsst2: Ki>5 μM; hsst3: Ki=1.4 μM; hsst5: Ki=0.54 μM) in Chinese hamster ovary (CHO) cells.