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

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.

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J-2156

J-2156 Estructura química

No. CAS : 848647-56-3

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Based on 1 publication(s) in Google Scholar

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Descripciòn

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].

MedChemExpress (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].

MedChemExpress (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.
Peso molecular

468.57

Fòrmula

C24H28N4O4S

No. CAS
Appearance

Solid

Color

White to off-white

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

DMSO : 200 mg/mL (426.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1342 mL 10.6708 mL 21.3415 mL 53.3538 mL
5 mM 0.4268 mL 2.1342 mL 4.2683 mL 10.6708 mL
10 mM 0.2134 mL 1.0671 mL 2.1342 mL 5.3354 mL
15 mM 0.1423 mL 0.7114 mL 1.4228 mL 3.5569 mL
20 mM 0.1067 mL 0.5335 mL 1.0671 mL 2.6677 mL
25 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
30 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7785 mL
40 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
50 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
60 mM 0.0356 mL 0.1778 mL 0.3557 mL 0.8892 mL
80 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6669 mL
100 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5335 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
J-2156
Cat. No.:
HY-111615
Cantidad:
MCE Japan Authorized Agent: