| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Cell death is induced in a dose- and time-dependent manner by EMD386088 (1, 10, 60 μM; 0-18 hours) [1]. EMD386088 (1, 10, 60 μM) both 5-HT6R-dependently and 5-HT6R-independently affects ERK1/2 activity [1].
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| ln Vivo |
In male Wistar rats, EMD386088 (1, 5, 10 mg/kg) reduced both long-term memory (LTM) and short-term memory (STM) at the 5 mg/kg dose but not at the 10 mg/kg level. impact [2]. The study found that EMD386088 (0, 2, 4 mg/kg) significantly reduced spontaneous alternation performance at the 2 mg/kg level. However, in C57BL/6J mice, the high dose of 4 mg/kg did not achieve statistical significance.
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| Cell Assay |
Cell viability assay [1]
Cell Types: HEK/HA-5-HT6R, native HEK293 Cell Tested Concentrations: 1, 10, 60 μM Incubation Duration: 0-18 hrs (hours) Experimental Results: Induced cells in HEK293 cells stably expressing HA-5-HT6R in dead (HEK/HA-5-HT6R) and native HEK293 cells in a dose- and time-dependent manner. Western Blot Analysis [1] Cell Types: HEK/HA-5-HT6R, native HEK293 Cell Tested Concentrations: 1, 10, 60 μM Incubation Duration: 0-18 h Experimental Results: 0-30 μM leads to ERK1/2 activation, in HEK/ In HA-5-HT6R cells, high doses of 60 μM delayed ERK1/2 activation. |
| References |
[1]. Yun HM, et al. 5-HT6 receptor ligands, EMD386088 and SB258585, differentially regulate 5-HT6 receptor-independent events. Toxicol In Vitro. 2011 Dec;25(8):2035-40.
[2]. Meneses A, et al. The effects of the 5-HT(6) receptor agonist EMD and the 5-HT(7) receptor agonist AS19 on memory formation. Behav Brain Res. 2008 Dec 16;195(1):112-9. [3]. Amodeo DA, et al. 5-HT6 receptor agonist EMD386088 impairs behavioral flexibility and working memory. Behav Brain Res. 2018 Sep 3;349:8-15. |
| Molecular Formula |
C14H15CLN2
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|---|---|
| Molecular Weight |
246.74
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| Exact Mass |
282.069
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| CAS # |
1171123-46-8
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| Related CAS # |
54635-62-0;
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| PubChem CID |
56972198
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.637
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
315
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.ClC1=CC=C2C(C(=C(N2)C)C2CCNCC=2)=C1
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| InChi Key |
WWSNDUWIZDYGIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15ClN2.ClH/c1-9-14(10-4-6-16-7-5-10)12-8-11(15)2-3-13(12)17-9;/h2-4,8,16-17H,5-7H2,1H3;1H
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| Chemical Name |
5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole;hydrochloride
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| Synonyms |
EMD386088; EMD 386088; EMD-386088
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.0528 mL | 20.2642 mL | 40.5285 mL | |
| 5 mM | 0.8106 mL | 4.0528 mL | 8.1057 mL | |
| 10 mM | 0.4053 mL | 2.0264 mL | 4.0528 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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