| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO: 100 mg/mL (171.65 mM) | [form ]
Solid | [color ]
White to off-white | [Water Solubility ]
Water: 100 mg/mL (171.65 mM) |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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] | [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[1]. | Animal Model: | Breast cancer-induced bone pain (BCIBP)-rats[1] | | Dosage: | 1, 3, 10?mg/kg | | Administration: | IP; for 3 hours | | Result: | Had anti-allodynic effect on ipsilateral and contralateral in BCIBP-rats.
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| [storage]
Store at -20°C | [References]
[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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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
| Company Name: |
MedChemExpress
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021-58955995 |
| Website: |
www.medchemexpress.com |
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