1. GPCR/G Protein
    Neuronal Signaling
  2. Somatostatin Receptor
  3. J-2156 TFA

J-2156 TFA 

Cat. No.: HY-111615A
Handling Instructions

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.

For research use only. We do not sell to patients.

J-2156 TFA Chemical Structure

J-2156 TFA Chemical Structure

CAS No. : 2387505-73-7

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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].

IC50 & 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.
Molecular Weight

582.59

Formula

C₂₆H₂₉F₃N₄O₆S

CAS No.

2387505-73-7

SMILES

O=C(N)[[email protected]@H](NC([[email protected]](CCN)NS(C1=CC=C(C)C2=CC=CC=C21)(=O)=O)=O)CC3=CC=CC=C3.O=C(O)C(F)(F)F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

J-2156J2156J 2156Somatostatin ReceptorSSTRsSSTRsomatostatinreceptortype4SST4mechanicalallodyniahyperalgesiaipsilateralhindpawsSST1SST2SST3SST5Inhibitorinhibitorinhibit

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J-2156 TFA
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