1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. 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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BW813U

BW813U Chemical Structure

CAS No. : 774142-74-4

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Description

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[1][2][3].

In Vitro

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.

In Vivo

BW813U (25-100 mg/kg/100 μM; i.p./bilateral intracranial injection; single injection) rapidly, dose-dependently and persistently inhibits brain ChAT activity in healthy male Sprague-Dawley rats[1].
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.

Animal Model: Sprague-Dawley (male, 325-375 g at study start)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg; 100 μM
Administration: i.p.; single injection; intracranial (bilateral); single injection
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.
Animal Model: Athymic mice[2]
Dosage: 2.5 mg/kg
Administration: i.p.; thrice a week
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.
Animal Model: Charles River CD (male, mature: 6-10 months, ~400 g; aged: 26-30 months, ~400 g)[3]
Dosage: 100 mg/kg
Administration: i.p.; single injection
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.
Molecular Weight

263.76

Formula

C15H18ClNO

CAS No.
SMILES

ClC1=CC=CC(/C=C/C2=NC(C)(C)CC(C)O2)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BW813U
Cat. No.:
HY-183572
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