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

J-2156 

Cat. No.: HY-111615
Handling Instructions

J-2156 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 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 Chemical Structure

J-2156 Chemical Structure

CAS No. : 848647-56-3

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Description

J-2156 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 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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

J-2156 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

468.57

Formula

C₂₄H₂₈N₄O₄S

CAS No.

848647-56-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (533.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1342 mL 10.6708 mL 21.3415 mL
5 mM 0.4268 mL 2.1342 mL 4.2683 mL
10 mM 0.2134 mL 1.0671 mL 2.1342 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

J-2156J2156J 2156Somatostatin ReceptorSSTRsSSTRsomatostatinreceptortype4SST4mechanicalallodyniahyperalgesiaipsilateralhindpawsSST1SST2SST3SST5Inhibitorinhibitorinhibit

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J-2156
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HY-111615
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