2387505-73-7
2387505-73-7 structure
- Name: J 2156
- Chemical Name: J-2156 TFA
- CAS Number: 2387505-73-7
- Molecular Formula: C26H29F3N4O6S
- Molecular Weight: 582.59
- Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
- Create Date: 2020-08-07 18:31:37
- Modify Date: 2024-01-22 13:01:04
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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 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2].
| Name | J-2156 TFA |
|---|
| Description | 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 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats[1][2]. |
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| Related Catalog | |
| Target |
IC50: 0.05 nM (human SST4) and 0.07 nM (rat SST4)[1] |
| In Vitro | J-2156 TFA binds with nanomolar affinity to the human somatostatin receptor subtype 4 (h sst4: Ki=1.2 nM) and is over 400-fold subtype-selective against the other somatostatin receptors (h sst1: Ki=1.2 nM; h sst2: Ki>5000 nM; h sst3: Ki=1400 nM; h sst5: Ki=540 nM) in Chinese hamster ovary (CHO) cells[2]. |
| 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. |
| References |
| Molecular Formula | C26H29F3N4O6S |
|---|---|
| Molecular Weight | 582.59 |