S 38093

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Cat.No. 6778 - S 38093 | C17H24N2O2 | CAS No. 1403835-45-9
Description: Selective H3 antagonist and inverse agonist; antinociceptive
Chemical Name: rel-4-[3-[(3aR,6aS)-Hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Selective H3 antagonist and inverse agonist (Ki values are 8.8, 1.2 and 1.44 μM, at rat, human and mouse respectively). Exhibits no activity at other histaminergic receptors. Antagonizes agonist action at mouse H3 receptors (KB = 0.65 μM). Exhibits inverse agonist action in cells expressing a high H3 receptor density, (EC50 values are 9 and 1.7 μM, at human and rat H3 receptors respectively). Exhibits antihyperalgesic effect in the Streptozocin-induced diabetic (STZ) neuropathy in vivo model. Promotes hippocampal neurogenesis in mouse model of Alzheimer's disease. Antinociceptive.

Technical Data

M. Wt 288.39
Formula C17H24N2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1403835-45-9
PubChem ID 70941112
InChI Key MRNMYWNBLVJWKG-GASCZTMLSA-N
Smiles [H][C@@]12CCC[C@@]1(CN(C2)CCCOC3=CC=C(C(N)=O)C=C3)[H]

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
DMSO 28.84 100
ethanol 14.42 50

Preparing Stock Solutions

The following data is based on the product molecular weight 288.39. 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 3.47 mL 17.34 mL 34.68 mL
5 mM 0.69 mL 3.47 mL 6.94 mL
10 mM 0.35 mL 1.73 mL 3.47 mL
50 mM 0.07 mL 0.35 mL 0.69 mL

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References

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

Guilloux et al (2017) S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci.Rep. 7 42946 PMID: 28218311

Chaumette et al (2018) Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur.J.Pain. 22 127 PMID: 28877402

Guilloux et al (2017) S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci.Rep. 7 42946 PMID: 28218311


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Keywords: S 38093, S 38093 supplier, S38093, H3, agonists, Receptors, Histamine, histaminergic, selective, antagonists, antagonism, inverse, agonism, antinociceptive, 6778, Tocris Bioscience

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