s38093 free
s38093 free Basic information
- Product Name:
- s38093 free
- Synonyms:
-
- s38093 free
- S38093 FREE BASE
- S-38093 free base
- S38093;S-38093;S 38093
- S38093;S-38093;S38093(FREE BASE)
- Benzamide, 4-[3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy]-
- 4-(3-(Hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide
- inhibit,S 38093,Histamine Receptor,Inhibitor
- CAS:
- 862896-30-8
- MF:
- C17H24N2O2
- MW:
- 288.38
- Product Categories:
-
- API
- Mol File:
- 862896-30-8.mol
s38093 free Chemical Properties
- Boiling point:
- 473.5±25.0 °C(Predicted)
- Density
- 1.130±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO : 15 mg/mL (52.01 mM)
- pka
- 16.34±0.50(Predicted)
- form
- Solid
- color
- White to off-white
s38093 free Usage And Synthesis
Uses
S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 μM for rat, mouse and human H3 receptors, respectively.
Biological Activity
S 38093 is a histamine H3 antagonist/inverse agonist with moderate affinity for rat, mouse and human H3 receptors (Ki values of 8.8, 1.44, 1.2 μM, respectively) and no affinity for other histaminergic receptors .
in vivo
S 38093 (0.3 and 3 mg/kg/d p.o., 28 days) significantly increases proliferation of progenitors in the DG of hippocampus in young adult mice. S 38093 (0.3 mg/kg/d) treatment significantly increases the number of DCX+ cells with tertiary dendrites. S 38093 (0.3, 1 and/or 3 mg/kg) significantly increases cell proliferation, survival, and maturation in the DG of hippocampus in aged mice relative to vehicle. S 38093 (3 mg/kg/d p.o., 28 days) increases cell proliferation and has a strong effect on cell survival, also increases the dendritic intersections in both genotypes (one-way ANOVA with repeated measure, p < 0.01), with a significant effect from 50 to 80 in APPSWETG mice only. In aged mice, chronic administration of S 38093 (1 and/or 3 mg/kg/day p.o., 28 days) reverses this age-dependent decrease in BDNF-IX, BDNF-IV and BDNF-I transcripts. In addition, S 38093 at three tested doses (0.3, 1 and 3 mg/kg/d) increases VEGF transcripts compared to vehicle-aged group[1]. In mice, S 38093 significantly increases ex vivo N-tele-Methylhistamine cerebral levels from 3 mg/kg p.o. and antagonized R-α-Methylhistamine-induced dipsogenia from 10 mg/kg i.p[2].
target
| Target | Value |
| human H3 receptor () | 1.2 μM(Ki) |
| mouse H3 receptor () | 1.44 μM(Ki) |
| rat H3 receptor () | 8.8 μM(Ki) |
IC 50
H3 receptor
References
[1] Guilloux JP, et al. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. DOI:10.1038/srep42946
[2] Sors A, et al. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23 DOI:10.1016/j.ejphar.2017.03.013
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