ABT-239
Based on 2 publication(s) in Google Scholar
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
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- Pureza: 99.23%
- No. CAS: 460746-46-7
- Fòrmula: C22H22N2O
- Peso molecular:330.42
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) ABT-239
MoreVer todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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H3 receptor |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | IC50 |
0.63 nM
Compound: 26, ABT-239
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Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
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[PMID: 18841880] |
Perfusion of the TMN with ABT-239 (10 μM) increases histamine release from the TMN, NBM, and cortex, but not from the striatum or NAcc. TMN perfusion with ABT-239 activates c-Fos selectively in the NBM and cortex[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 460746-46-7
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Appearance Solid
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Peso molecular 330.42
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Fòrmula C22H22N2O
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Color Light yellow to khaki
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SMILES
C[C@H]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1
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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 (2)
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Journal Impact Factor
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Most Recent
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Pharmaceuticals (Basel)
Anti-COVID Drugs (MMV COVID Box) as Leishmanicidal Agents: Unveiling New Therapeutic Horizons. [Abstract]2024 Feb 20;17(3):266. PMID: 38543052 -
Int J Parasitol Drugs Drug Resist
Exploring therapeutic approaches against Naegleria fowleri infections through the COVID box. [Abstract]2024 Aug:25:100545. PMID: 38718717
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (302.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 (7.57 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 (7.57 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocolo
Solutions of KA, ABT-239 and SVP are prepared in pyrogen-free normal saline for injection except for TDZD-8, which is dissolved in 10% DMSO and are administered intraperitoneally in a volume not exceeding 10 mL/kg. The animals are divided into ten groups. The first group (CTRL) receive vehicle (0.9% sodium chloride) only whereas animals in the second group (VEH) are given vehicle followed by KA at a dose of 10 mg/kg, i.p. (pH 7.2±1), this being the dose that induces low-grade seizures (stage 0-4) in all the animals without any mortality in a range finding study. The KA dose employs to evoke SE in mice in various studies mostly varied from as low as 6-20 mg/kg to as high as 25-45 mg/kg. Animals in the next two groups are administered ABT-239 in increasing doses of 1 (AL) and 3 mg/kg (AH) 30 min before KA challenge. These doses ranging from 0.1 to 3 mg/kg of ABT-239 display disease modifying attributes in a mice model of Alzheimer׳s disease as well as improved cognitive functions. The fifth and sixth group receive graduated doses of 150 (SL) and 300 mg/kg (SH) of SVP 30 min prior to KA injection. The seventh and eight group receive combinations of subeffective dose (maximum possible dose at which there is no protection) of SVP at 150 mg/kg with ABT-239 at 1 (SLAL) and 3 mg/kg (SLAH) respectively followed 30 min later by KA. The remaining two groups receive low dose combination at 1 and 5 mg/kg (ALTL) and a high dose combination at 3 and 10 mg/kg (AHTH) of ABT-239 and TDZD-8, respectively before KA exposure. The doses of TDZD-8 chosen are based on previous studies where doses ranging from 1 to 10 mg/kg reduced inflammation and tissue injury as well as improve psychiatric conditions.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bhowmik M, et al. Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40. [Content Brief]
[2]. Provensi G, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H3 receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacolo [Content Brief]
[3]. Kruk M, e tal. Effects of the histamine H2 receptor antagonist ABT-239 on cognition and nicotine-induced memory enhancement in mice. Pharmacol Rep. 2012;64(6):1316-25. [Content Brief]
[4]. Munari L, et al. Selective brain region activation by histamine H2 receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40. [Content Brief]
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 | 3.0265 mL | 15.1323 mL | 30.2645 mL | 75.6613 mL |
| 5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL | 15.1323 mL | |
| 10 mM | 0.3026 mL | 1.5132 mL | 3.0265 mL | 7.5661 mL | |
| 15 mM | 0.2018 mL | 1.0088 mL | 2.0176 mL | 5.0441 mL | |
| 20 mM | 0.1513 mL | 0.7566 mL | 1.5132 mL | 3.7831 mL | |
| 25 mM | 0.1211 mL | 0.6053 mL | 1.2106 mL | 3.0265 mL | |
| 30 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5220 mL | |
| 40 mM | 0.0757 mL | 0.3783 mL | 0.7566 mL | 1.8915 mL | |
| 50 mM | 0.0605 mL | 0.3026 mL | 0.6053 mL | 1.5132 mL | |
| 60 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL | |
| 100 mM | 0.0303 mL | 0.1513 mL | 0.3026 mL | 0.7566 mL |
ABT-239 Related Classifications
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