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| 25mg |
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Purity: ≥98%
S 38093 is a novel brain-penetrant antagonist (inverse agonist) of the H3 (histamine H3) receptor with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively. It may provide an innovative strategy to improve age-associated cognitive deficits. In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65 µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11 µM). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7 µM, respectively). S 38093, as a novel H3 inverse agonist, is a good candidate for further in vivo evaluations, in particular in animal models of cognition.
| ln Vitro |
In cell models, S 38093 antagonizes mouse H3 receptors (KB=0.65 µM) and inhibits H3 agonists through human H3 receptors (KB=0.11 µM). In cells expressing high H3 densities, S 38093 functions as a mild inverse agonist at rat and human H3 receptors (EC50 9 µM and 1.7 µM, respectively) [2].
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| ln Vivo |
In the hippocampus DG of young adult mice, 38093 (0.3 and 3 mg/kg/d, oral, 28 days) markedly boosted the proliferation of progenitor cells. The number of DCX+ cells with third-order dendrites was dramatically increased upon treatment with S 38093 (0.3 mg/kg/d). S 38093 (0.3, 1 and/or 3 mg/kg) dramatically enhanced cell proliferation, survival, and maturation in the DG of the hippocampus regions of aged mice as compared to vehicle. Only in APPSWETG mice did S 38093 (3 mg/kg/d, po, 28 days) have a significant effect from 50 to 80. It also boosted dendritic crossing and had a robust effect on cell survival in both genotypes (one-way ANOVA with repeated measures, p < 0.01). Chronic delivery of S 38093 (1 and/or 3 mg/kg/day, po, for 28 days) corrected this age-dependent reduction in the transcripts of BDNF-IX, BDNF-IV, and BDNF-I in elderly mice. Furthermore, in comparison to the vehicle aging group, S 38093 enhanced VEGF transcripts at three tested doses (0.3, 1 and 3 mg/kg/d) [1]. At an oral dose of 3 mg/kg, S 38093 markedly elevated ex vivo N-tele-Mmethylhistamine levels in the mouse brain. A 10 mg/kg intraperitoneal injection can counteract the addictive effects of R-α-methylhistamine [2].
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| References |
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| Molecular Formula |
C17H25CLN2O2
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| Molecular Weight |
324.85
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| Exact Mass |
324.16
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| Elemental Analysis |
C, 62.86; H, 7.76; Cl, 10.91; N, 8.62; O, 9.85
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| CAS # |
1222097-72-4
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| Related CAS # |
S 38093;862896-30-8
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| PubChem CID |
45280145
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
341
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O(C1C=CC(C(N)=O)=CC=1)CCCN1CC2CCCC2C1
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| InChi Key |
AFSVOZDCVFYWFG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H24N2O2.ClH/c18-17(20)13-5-7-16(8-6-13)21-10-2-9-19-11-14-3-1-4-15(14)12-19;/h5-8,14-15H,1-4,9-12H2,(H2,18,20);1H
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| Chemical Name |
4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0783 mL | 15.3917 mL | 30.7834 mL | |
| 5 mM | 0.6157 mL | 3.0783 mL | 6.1567 mL | |
| 10 mM | 0.3078 mL | 1.5392 mL | 3.0783 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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