Basmisanil
Based on 1 publication(s) in Google Scholar
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.40%
- No. CAS: 1159600-41-5
- Fòrmula: C21H20FN3O5S
- Peso molecular:445.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Publications Citing Use of MedChemExpress (MCE) Basmisanil
More
Actividad biológica
IC50: 8 nM (GABAAα5)
Ki: 5 nM (GABAAα5); 1031 nM (GABAAα1); 458 nM (GABAAα2); 510 nM (GABAAα3)
Basmisanil (0.1 nM-100 μM) has high affinity for bounding to recombinant human GABAA-α5 receptors with a Ki value of 5 nM and more than 90-fold selectivity versus α1 (Ki = 1031 nM), α2 (Ki = 458 nM), and α3 (Ki = 510 nM) subunit-containing receptors[1].
Basmisanil (1 nM-1 μM) shows a highly selective inhibition of GABAA-α5 with a IC50 value of 8 nM[1].
Basmisanil (1 μM) inhibits GABA-induced currents at GABAA-α5 yet had little or no effect at the other receptor subtypes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Basmisanil (3-600 mg/kg p.o.) improves cognition in rats and non.human primates and not show anxiogenic or proconvulsant effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats[1]
(180 g; female) -
Dosage:3-100 mg/kg
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Administration:p.o.
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Result:Decreased the binding of [3H]-Ro 15-4513 in a dose-dependent manner.
Reduced specific binding in the hippocampus by 70% at the highest dose (100 mg/kg).
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Animal Model:Lister Hooded rats, Wistar rats and F-344 Fischer rats [1]
(Lister Hooded rats: 220-250 g; male)
(Wistar rats: 200-220 g; male and female)
(F-344 Fischer rats: 170-180 g; male) -
Dosage:3-600 mg/kg
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Administration:p.o.
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Result:Significantly attenuated the diazepam-induced deficit.
Showed plasma concentrations in dose- and time-dependent manner and reached a maximal level of 903 ng/mL (379 nM free plasma) 30 min after the administration at 10 mg/kg.
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Animal Model:Male cynomolgus macaques[1]
(Macaca fascicularis; 7-10 kg) -
Dosage:1-600 mg/kg
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Administration:p.o.
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Result:Significantly improved the percentage of correct first reaches during difficult trials of the object retrieval task at the 3 and 10 mg/kg doses.
Exhibited an inverted U-shaped dose response in this paradigm with the 1 and 30 mg/kg doses producing no marked improvement on performance.
Increased the total plasma exposure in dose-dependent.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1159600-41-5
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Appearance Solid
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Peso molecular 445.46
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Fòrmula C21H20FN3O5S
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Color White to off-white
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SMILES
O=C(N1CCS(CC1)(=O)=O)C2=CC=C(OCC3=C(C)ON=C3C4=CC=C(F)C=C4)N=C2
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Synonyms
RG1662; RO5186582
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Neuropharmacology
2019 May 1:149:161-168. PMID: 30797029
Solvente y solubilidad
DMSO : 100 mg/mL (224.49 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2449 mL | 11.2244 mL | 22.4487 mL | 56.1218 mL |
| 5 mM | 0.4490 mL | 2.2449 mL | 4.4897 mL | 11.2244 mL | |
| 10 mM | 0.2245 mL | 1.1224 mL | 2.2449 mL | 5.6122 mL | |
| 15 mM | 0.1497 mL | 0.7483 mL | 1.4966 mL | 3.7415 mL | |
| 20 mM | 0.1122 mL | 0.5612 mL | 1.1224 mL | 2.8061 mL | |
| 25 mM | 0.0898 mL | 0.4490 mL | 0.8979 mL | 2.2449 mL | |
| 30 mM | 0.0748 mL | 0.3741 mL | 0.7483 mL | 1.8707 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4030 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1224 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9354 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5612 mL |
Basmisanil Related Classifications
HY-16716 Related Classifications
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