ABT-239, inhibitor

ABT-239

Cat. Num. AAA5754466

• Purity: 98.00%
• Synonyms: ABT-239; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (302.65mM); H2O: <0.1mg/mL (insoluble); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C22H22N2O
• SMILES: C[C@H]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1
• CAS Number: 460746-46-7
• Target & IC50: Others
• In Vitro: ABT-239 (3mg/kg, i.p.) significantly delays onset of seizure, reduces behavioral seizures elicited by KA, and reduces in the incidence of head bobbing and forelimb clonus in mice. ABT-239 (3mg/kg, i.p.) administration transforms a short-term learning event into a long-term remembered experience in WT but not in histamine-depleted mice[2]. ABT-239 (3mg/kg, i.p.) causes enhanced reduction in all the stages. ABT-239 (3mg/kg, i.p.) and TDZD-8 (10mg/kg, i.p.) have more powerful reduction in the number of pyknotic neurons in mice hippocampi. ABT-239 (1mg/kg, i.p.) in conbination with sub-therapeutic dose of SVP (150mg/kg, i.p.), significantly decreases the number of immobility, head bobbing and forelimb clonus, where as a higher dose combination of The high dose combination of ABT-239 and TDZD-8 produces the most pronounced increase in Bcl-2 expression as well as decrease in the level of Bax[1]. Concomitant administration of either ABT-239 (1 and 3mg/kg, i.p.) and nicotine (0.035mg/kg, i.p.), or ABT-239 (0.1mg/kg, i.p.) and nicotine (0.0175mg/kg, i.p.) further increases nicotine-induced improvement in both memory acquisition and consolidation[3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for ABT-239, inhibitor

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist. Its a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

References

Bhowmik M, et al. histamine H receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.
Bhowmik M, et al. histamine H receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep 18;1581:129-40.
Provensi G, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacolo
Provensi G, et al. Donepezil, an acetylcholine esterase inhibitor, and ABT-239, a histamine H receptor antagonist/inverse agonist, require the integrity of brain histamine system to exert biochemical and procognitive effects in the mouse. Neuropharmacolo
Kruk M, e tal. Effects of the histamine H receptor antagonist ABT-239 on cognition and nicotine-induced memory enhancement in mice. Pharmacol Rep. 2012;64(6):1316-25.
Kruk M, e tal. Effects of the histamine H receptor antagonist ABT-239 on cognition and nicotine-induced memory enhancement in mice. Pharmacol Rep. 2012;64(6):1316-25.
Munari L, et al. Selective brain region activation by histamine H receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40.
Munari L, et al. Selective brain region activation by histamine H receptor antagonist/inverse agonist ABT-239 enhances acetylcholine and histamine release and increases c-Fos expression. Neuropharmacology. 2013 Jul;70:131-40.