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GSK189254A

Catalog No. TQ0066   CAS 720690-73-3
Synonyms: GSK189254

GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).

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GSK189254A Chemical Structure
GSK189254A, CAS 720690-73-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 85.00
10 mg In stock $ 126.00
50 mg In stock $ 369.00
100 mg In stock $ 531.00
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Purity: 98.71%
Purity: 98.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).
Targets&IC50 mouse H3 receptor:8.51-9.17 (pKi), human H3 receptor:9.59-9.90 (pKi)
In vitro GSK189254 has a high affinity for both recombinant H3 receptors expressed in HEK-293-MSR-II cells and native H3 receptors expressed in the cerebral cortex of several species. GSK189254 generally exhibits a higher affinity for human and pig H3 receptors compared with mouse, rat, and dog H3 receptors. GSK189254 may have therapeutic potential for the symptomatic treatment of dementia in Alzheimer’s disease and other cognitive disorders [1].
In vivo In Ox+/+ and Ox?/? mice, acute administration of GSK189254 increases W and decreases slow wave and paradoxical sleep to a similar degree to modafinil, while it reduces narcoleptic episodes in Ox?/? mice [2]. GSK189254 (0.3-3 mg/kg p.o.) increases the release of acetylcholine, noradrenaline, and dopamine in the anterior cingulate cortex and acetylcholine in the dorsal hippocampus. GSK189254 significantly improves the performance of rats in diverse cognition paradigms, including passive avoidance, water maze, object recognition, and attentional set shift [1].
Animal Research Pharmacokinetic studies with GSK189254 are conducted in conscious male Sprague-Dawley rats. Animals receive an intravenous infusion of GSK189254 (n=3) administered at a nominal dose level of 1 mg of free base/kg for 1 h via the femoral vein cannula (10 mL/h/kg). GSK189254 is dissolved in 0.9% (w/v) saline at a target concentration of 0.1 mg free base/mL and filtered with a 0.22-mm Millex-GV filter before administration. After an ish out of at least 2 days, the same rats received a single oral administration of GSK189254 by gastric gavage to achieve a target dose of 2 mg of free base/kg. GSK189254 is formulated in 1% (w/v) aqueous methylcellulose at a target concentration of 0.4 mg free base/mL [1]. The vehicle consists of 0.05 mL NaCl at 0.9% containing methylcellulose at 1%. GSK189254 is a dissolved in-vehicle solution. The effects of acute and repeat administration of GSK189254 on the sleep-wake cycle in wild-type (Ox+/+) and orexin knockout (Ox?/?) mice is investigated. GSK189254 (3 and 10 mg/kg, p.o.) is administered on the sleep-wake cycle in Ox+/+ and Ox?/? mice, dosed at 10 h. The oral administration dose of GSK189254 is 10 mg/kg [2].
Synonyms GSK189254
Molecular Weight 351.44
Formula C21H25N3O2
CAS No. 720690-73-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 24 mg/mL (68.29 mM), sonification is recommended.

TargetMolReferences and Literature

1. Medhurst AD, et al. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. 2. Guo RX, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.Br J Pharmacol. 2009 May;157(1):104-17.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Parkinson's Disease Compound Library Drug Repurposing Compound Library Immunology/Inflammation Compound Library Inhibitor Library Bioactive Compounds Library Max Clinical Compound Library Bioactive Compound Library

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Keywords

GSK189254A 720690-73-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor GSK-189254A inhibit GSK-189254 GSK189254 GSK 189254 Inhibitor inhibitor

 

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