Samelisant
Based on 1 Customer Validation
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
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- Pureza: 98.65%
- No. CAS: 1394808-20-8
- Fòrmula: C21H33Cl2N3O3
- Peso molecular:446.41
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
20 nM
Compound: 17v
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Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay
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[PMID: 30629436] |
| HEK293 | IC50 |
>10 μM
Compound: 17v
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Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp assay
Inhibition of human ERG expressed in HEK293 cells by whole-cell patch clamp assay
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[PMID: 30629436] |
Samelisant displays inverse agonist activity and it exhibits very high selectivity towards H3R. The pEC50 value of histamine (8.5) for human H3 receptor increases to 8.2, 7.3 and 6.2 after treatment with 1, 10 and 100 nM of Samelisant, respectively. The pEC50 value of histamine (8.2) for rat H3 receptor increases to 7.9, 7.4 and 6.4 after treatment with 1, 10 and 100 nmol/L of Samelisant, respectively[1].
Samelisant binds to the orthosteric site in a reversible manner with Kb values of 1.3 nM and 1.1 nM deduced from pA2 value for human and rat H3R, respectively[1].
Samelisant also modulates dopamine and norepinephrine levels in the cerebral cortex while it has no effects on dopamine levels in the striatum or nucleus accumbens[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Samelisant also produces a significant decrease in direct rapid eye movement (REM) sleep onset (DREM) episodes, demonstrating its anticataplectic effects in an animal model relevant to narcolepsy[1].
Samelisant treatment in mice produces a dose-dependent increase in tele-methylhistamine levels indicating the activation of histaminergic neurotransmission[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats or male C57BL6J mice[1]
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Dosage:1, 3, 10, and 30 mg/kg
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Administration:Oral administration
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Result:Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats. Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1394808-20-8
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Appearance Solid
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Peso molecular 446.41
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Fòrmula C21H33Cl2N3O3
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Color Off-white to light yellow
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SMILES
O=C(CN1CCOCC1)NC2=CC=C(C=C2)OC3CCN(CC3)C4CCC4.[H]Cl.[H]Cl
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Synonyms
SUVN-G3031
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 62.5 mg/mL (140.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2401 mL | 11.2005 mL | 22.4009 mL | 56.0023 mL |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4802 mL | 11.2005 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2401 mL | 5.6002 mL | |
| 15 mM | 0.1493 mL | 0.7467 mL | 1.4934 mL | 3.7335 mL | |
| 20 mM | 0.1120 mL | 0.5600 mL | 1.1200 mL | 2.8001 mL | |
| 25 mM | 0.0896 mL | 0.4480 mL | 0.8960 mL | 2.2401 mL | |
| 30 mM | 0.0747 mL | 0.3733 mL | 0.7467 mL | 1.8667 mL | |
| 40 mM | 0.0560 mL | 0.2800 mL | 0.5600 mL | 1.4001 mL | |
| 50 mM | 0.0448 mL | 0.2240 mL | 0.4480 mL | 1.1200 mL | |
| 60 mM | 0.0373 mL | 0.1867 mL | 0.3733 mL | 0.9334 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2800 mL | 0.7000 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5600 mL |
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