產(chǎn)品屬性：
產(chǎn)品名稱 | J-2156 TFA |
規(guī)格 | 10mM*1 mL in DMSO、5 mg、10 mg、25 mg、50 mg、100 mg |
貨號 | EY-01Y12187 |
Cas No.: 2387505-73-7
別名: N/A
化學(xué)名: N/A
分子式: C26H29F3N4O6S
分子量: 582.59
溶解度: H2O: 100 mg/mL (171.65 mM); DMSO: 100 mg/mL (171.65 mM)
儲存條件: Store at -20°C, protect from light, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
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[1][2].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[2].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][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.
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