J 2156

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Cat.No. 6201 - J 2156 | C24H28N4O4S.C2HF3O2
Description: Selective high affinity human sst4 agonist
Chemical Name: (1'S,2S)-4-Amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4"-methyl-1"-naphthalenesulfonylamino)butanamide trifluoroacetate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

High affinity human somatostatin receptor 4 (sst4) agonist (Ki = 1.2 nM). Displays >400-fold selectivity for human sst4 over other human sst receptor subtypes. Exhibits 2 to 3-fold more potent agonism in vitro than endogenous ligands somatostatin-14 (Cat. No. 1157) and somatostatin-28 (Cat. No. 1165). Reduces inflammatory airway hyperresponsiveness in acute and chronic airway inflammation models in mice. Exhibits anxiolytic effects in elevated plus maze test in mice.

Technical Data

M. Wt 582.6
Formula C24H28N4O4S.C2HF3O2
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 11442741
InChI Key VTNCZBXJSGKDLS-SFTDATJTSA-N
Smiles CC1=CC=C(S(=O)(N[C@H](C(N[C@H](C(N)=O)CC2=CC=CC=C2)=O)CCN)=O)C3=C1C=CC=C3.OC(C(F)(F)F)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 58.26 100
DMSO 58.26 100

Preparing Stock Solutions

The following data is based on the product molecular weight 582.6. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.72 mL 8.58 mL 17.16 mL
5 mM 0.34 mL 1.72 mL 3.43 mL
10 mM 0.17 mL 0.86 mL 1.72 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References

References are publications that support the biological activity of the product.

Engström et al (2005) Superagonism at the human somatostatin receptor subtype 4. J.Pharmacol.Exp.Ther. 312 332 PMID: 15333679

Elekes et al (2008) Inhibitory effects of synthetic somatostatin receptor subtype 4 agonists on acute and chronic airway inflammation and hyperreactivity in the mouse. Eur.J.Pharmacol. 578 313 PMID: 17961545

Scheich et al (2016) Somatostatin receptor subtype 4 activation is involved in anxiety and depression-like behavior in mouse models. Neuropharmacology. 101 204 PMID: 26387439


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Keywords: J 2156, J 2156 supplier, J2156, human, somatostatin, receptor, 4, sst4, superagonist, agonists, agonism, 848647-56-3, anti-inflammatory, Somatostatin, Receptors, 6201, Tocris Bioscience

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