| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist/inverse agonist developed by Abbott with stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia. ABT-239 exhibits greater activity at the human H3 receptor in comparison to similar agents like ciproxifan, thioperamide, and cipralisant.
| Targets |
H3 receptor
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|---|---|
| ln Vitro |
ABT-239 (10 μM) perfusion of the TMN increases the release of histamine from the TMN, NBM, and cortex, but not from the striatum or NAcc. In the NBM and cortex, TMN perfusion combined with ABT-239 selectively activates c-Fos[4].
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| ln Vivo |
ABT-239 (3 mg/kg, i.p.) dramatically postpones the onset of seizures, decreases behavioral seizures induced by KA, and lowers the frequency of head bobbing and forelimb clonus in mice. In contrast, a higher dose combination of ABT-239 (3 mg/kg, i.p.) results in enhanced reduction in all stages of immobility, head bobbing, and forelimb clonus. ABT-239 (1 mg/kg, i.p.) and sub-therapeutic dose of SVP (150 mg/kg, i.p.) significantly reduce these symptoms. In mice, the number of pyknotic neurons in the hippocampi is more effectively reduced by ABT-239 (3 mg/kg, i.p.) and TDZD-8 (10 mg/kg, i.p.). The strongest increase in Bcl-2 expression and lowest level of Bax are produced by the high dose combination of ABT-239 and TDZD-8[1]. In WT mice, but not in histamine-depleted mice, ABT-239 (3 mg/kg, i.p.) administration creates long-term memories from short-term learning events[2]. The enhancement of nicotine-induced memory acquisition and consolidation is further enhanced by the concurrent administration of ABT-239 (1 and 3 mg/kg, i.p.) and nicotine (0.035 mg/kg, i.p.) or ABT-239 (0.1 mg/kg, i.p.) and nicotine (0.0175 mg/kg, i.p.)[3].
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| Animal Protocol |
ABT-239, SVP, and KA solutions are made in pyrogen-free normal saline for injection; TDZD-8, on the other hand, is dissolved in 10% DMSO and injected intraperitoneally in a volume not to exceed 10 mL/kg. There are ten groupings of animals. In a range finding study, animals in the second group (VEH) receive KA at a dose of 10 mg/kg, i.p. (pH 7.2±1), while the first group (CTRL) receives only vehicle (0.9% sodium chloride). This dose causes low-grade seizures (stages 0-4) in all animals without causing any mortality. In most studies, the KA dose used to elicit SE in mice ranged from 6–20 mg/kg to 25–45 mg/kg and higher. Two groups of animals receive increasing doses of ABT-239 (30 min before KA challenge): 1 mg/kg (AL) and 3 mg/kg (AH). In mice with Alzheimer's disease, these doses of ABT-239, which range from 0.1 to 3 mg/kg, show improved cognitive functions as well as disease-modifying properties. Prior to the KA injection, 30 minutes are spent giving the fifth and sixth groups graduated doses of SVP at 150 (SL) and 300 mg/kg (SH). The subeffective dose (the highest dose at which no protection is possible) of SVP at 150 mg/kg combined with ABT-239 at 1 (SLAL) and 3 mg/kg (SLAH), respectively, is given to the seventh and eighth groups. Thirty minutes later, KA administers the combination. Before being exposed to KA, the remaining two groups receive low doses of ABT-239 and TDZD-8, respectively, at 1 and 5 mg/kg (ALTL) and high doses, at 3 and 10 mg/kg (AHTH). The TDZD-8 dosages selected are based on earlier research in which doses between 1 and 10 mg/kg improved psychiatric conditions and decreased inflammation and tissue damage.
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| References |
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| Molecular Formula |
C22H22N2O
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|---|---|
| Molecular Weight |
330.42288
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| Exact Mass |
330.173
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| Elemental Analysis |
C, 79.97; H, 6.71; N, 8.48; O, 4.84
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| CAS # |
460746-46-7
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| PubChem CID |
9818903
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
4.936
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
490
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| Defined Atom Stereocenter Count |
1
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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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| InChi Key |
KFHYZKCRXNRKRC-MRXNPFEDSA-N
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| InChi Code |
InChI=1S/C22H22N2O/c1-16-3-2-11-24(16)12-10-21-14-20-13-19(8-9-22(20)25-21)18-6-4-17(15-23)5-7-18/h4-9,13-14,16H,2-3,10-12H2,1H3/t16-/m1/s1
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| Chemical Name |
4-[2-[2-[(2R)-2-methylpyrrolidin-1-yl]ethyl]-1-benzofuran-5-yl]benzonitrile
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| Synonyms |
ABT-239; ABT 239; ABT239
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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) |
DMSO: ≥ 100 mg/mL (~302.7 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.57 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0265 mL | 15.1323 mL | 30.2645 mL | |
| 5 mM | 0.6053 mL | 3.0265 mL | 6.0529 mL | |
| 10 mM | 0.3026 mL | 1.5132 mL | 3.0265 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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