BW813U
BW813U is a blood-brain barrier-permeable choline acetyltransferase (ChAT) inhibitor. BW813U reduces acetylcholine secretion, decreases cancer cell viability, and slows tumor growth rate. BW813U alters reference memory and causes working memory dysfunction. BW813U shows a synergistic effect with age factors in memory deficits of rats. BW813U can be used in studies related to Alzheimer's disease and lung cancer.
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- CAS No.: 774142-74-4
- Formule: C15H18ClNO
- Masse moléculaire:263.76
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
BW813U potently reduces the viability of human SCC-L and LAC cell lines in vitro in a concentration-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BW813U (2.5 mg/kg; i.p.; three times per week) potently reduces the growth rate of xenografted H838 human lung adenocarcinoma tumors in athymic mice without causing obvious toxicity[2].
BW813U (100 mg/kg; i.p.; single administration) causes a synergistic prolongation of peak latency in rats with increasing age, indicating impaired reference memory; it also eliminates memory retention of pre-gap signal duration in the PI-GAP test, indicating impaired working memory for temporal information[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 325-375 g at study start)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg; 100 μM
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Administration:i.p.; single injection; intracranial (bilateral); single injection
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Result:Caused 60% decrease in cortex, 48% decrease in hippocampus, and 70% decrease in caudate nucleus ChAT activity 1 hour post-injection.
Caused a rapid decrease in ChAT activity, with 45% decrease in cortex and 55% decrease in hippocampus at day 1, persisting (with partial recovery) through day 19.
Caused 78% decrease in cortex, 68% decrease in hippocampus, and 85% decrease in caudate nucleus ChAT activity 1 hour post-injection.
Caused sustained ChAT inhibition for 1 week post-injection.
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Animal Model:Athymic mice[2]
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Dosage:2.5 mg/kg
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Administration:i.p.; thrice a week
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Result:Robustly decreased the growth rate of H838 human LAC tumors.
No gross toxicity, behavioral discomfort, or differences in body weight, food consumption, or water consumption were observed between BW813U-treated and vehicle-treated mice.
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Animal Model:Charles River CD (male, mature: 6-10 months, ~400 g; aged: 26-30 months, ~400 g)[3]
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Dosage:100 mg/kg
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Administration:i.p.; single injection
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Result:Increased mean peak time to 22.3 s in mature rats (vs 20.6 s in vehicle controls) in post-drug PI testing.
Increased mean peak time to 30.25 s in aged rats (vs 24.6 s in vehicle controls) in post-drug PI testing.
Increased mean peak time on gap trials by 15.8 s in mature rats (vs 6.0 s in vehicle controls) in post-drug PI-GAP testing.
Increased mean peak time on gap trials by 16.4 s in aged rats (vs 6.5 s in vehicle controls) in post-drug PI-GAP testing.
Showed no significant differences in peak rate and coefficient of variation measures compared to vehicle groups in post-drug PI testing.
Showed no significant differences in peak rate measures between probe trials with and without gaps.
Chemical Information
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CAS No. 774142-74-4
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Masse moléculaire 263.76
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Formule C15H18ClNO
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SMILES
ClC1=CC=CC(/C=C/C2=NC(C)(C)CC(C)O2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Wenk G, et al. Cholinergic function and memory: extensive inhibition of choline acetyltransferase fails to impair radial maze performance in rats. Pharmacol Biochem Behav. 1986;25(3):521-526. [Content Brief]
[2]. Friedman JR, et al. Acetylcholine signaling system in progression of lung cancers. Pharmacol Ther. 2019 Feb;194:222-254. [Content Brief]
[3]. Meck WH, et al. Temporal memory in mature and aged rats is sensitive to choline acetyltransferase inhibition. Brain Res. 2006;1108(1):168-175. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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