CAS NO: | 2387505-73-7 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 2387505-73-7 |
分子式 | C26H29F3N4O6S |
分子量 | 582.59 |
溶解度 | Water: 100 mg/mL (171.65 mM); DMSO: 100 mg/mL (171.65 mM) |
储存条件 | Store at -20°C, protect from light, stored under nitrogen |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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 (1-10mg/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 EngstrÖm, et al. Superagonism at the Human Somatostatin Receptor Subtype 4. J Pharmacol Exp Ther. 2005 Jan;312(1):332-8. |