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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 might offer a novel approach to addressing age-related cognitive impairments. S 38093 can suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11 µM) and antagonize mice H3 receptors (KB=0.65 µM) in cellular models. S 38093 acts as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7 µM, respectively) in cells expressing a high density of H3. S 38093 is a promising candidate for additional in vivo testing as a novel H3 inverse agonist, especially in animal models of cognition.
| Targets |
Rat H3 receptor ( Ki = 8.8 µM ); Mouse H3 receptor ( Ki = 1.44 µM ); Human H3 receptor ( Ki = 1.2 µM )
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| ln Vitro |
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| Enzyme Assay |
S 38093 is a new type of inverse agonist that selectively blocks the H3 (histamine H3) receptor in the brain. Its Ki values for rat, mouse, and human H3 receptors are 8.8, 1.44, and 1.2 µM, respectively.
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| Cell Assay |
After being harvested at a density of 2 x 106 cells per milliliter, the cells were suspended in Hank's balanced salt solutions/HEPES (pH7.4) buffer, which contained 1 mM isobutyl-methylxanthine and 1 mg/ml BSA. After adding 1 μl of the fluor 647-anti-cAMP antibody solution to 100 μl of the cell suspension, 6 μl aliquots of the mixture were put into white 384-well microtiter plates. Then, in order to preactivate adenylate cyclase, the cells were incubated with 6 μl aliquots of S 38093 and/or the reference compounds (specific H3 agonist Imetit or antagonist Thioperamide) at increasing concentrations (0.01-100 μM), in the presence of forskolin (FSK, 0.5 μM final concentration). The cells were treated with the lysis buffer (0.35% Triton X-100, 10mM CaCl2, 50mM HEPES) containing LANCE EU-W8044 labeled streptavidin and biotinyled cAMP after a one-hour incubation period at room temperature in the dark. Plates were read on a microplate reader following a 20-hour dark incubation period at +4°C.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C17H24N2O2
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| Molecular Weight |
288.384664535522
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| Exact Mass |
288.18
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| Elemental Analysis |
C, 70.80; H, 8.39; N, 9.71; O, 11.10
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| CAS # |
862896-30-8
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| Related CAS # |
S 38093 hydrochloride; 1222097-72-4
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| PubChem CID |
11380684
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| Appearance |
White to off-white solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
341
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MRNMYWNBLVJWKG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H24N2O2/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)
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| Chemical Name |
4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide
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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 | 3.4676 mL | 17.3382 mL | 34.6765 mL | |
| 5 mM | 0.6935 mL | 3.4676 mL | 6.9353 mL | |
| 10 mM | 0.3468 mL | 1.7338 mL | 3.4676 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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