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

J-2156 TFA 

Cat. No.: HY-111615A Purity: 99.98%
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 has anti-inflammatory activity and it 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.

Custom Peptide Synthesis

J-2156 TFA Chemical Structure

J-2156 TFA Chemical Structure

CAS No. : 2387505-73-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 256 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 256 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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 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].

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 (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].

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

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].

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

582.59

Formula

C₂₆H₂₉F₃N₄O₆S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Protect from light, stored under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (171.65 mM; Need ultrasonic)

DMSO : 100 mg/mL (171.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7165 mL 8.5824 mL 17.1647 mL
5 mM 0.3433 mL 1.7165 mL 3.4329 mL
10 mM 0.1716 mL 0.8582 mL 1.7165 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: ≥ 2.5 mg/mL (4.29 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.29 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
J-2156 TFA
Cat. No.:
HY-111615A
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