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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 774142-74-4
- Formel: C15H18ClNO
- Molecular Weight:263.76
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
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.
-
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.
Chemical Information
-
CAS. Nr. 774142-74-4
-
Molecular Weight 263.76
-
Formel C15H18ClNO
-
SMILES
ClC1=CC=CC(/C=C/C2=NC(C)(C)CC(C)O2)=C1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BW813U Related Classifications
HY-183572 Related Classifications
Powered by Bioz