Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1]. |
Targets&IC50 | BACE1:9.1 nM , Cellular β-Amyloid:0.82 nM |
In vivo | Treatment with BACE1-IN-5 (Compound 15), administered orally at doses ranging from 1-3 mg/kg to male ICR mice for durations of 2-6 hours, significantly and dose-dependently decreases total amyloid-beta (Aβ) levels. At a dose of 1 mg/kg, it reduces total Aβ by 76% within 4 hours, correlating with a free brain concentration of 4.1 ng/mL (8.9 nM). This compound also exhibits a K_p,uu value of 1.3 at the 4-hour mark and a 1 mg/kg dose. When the dosage is increased to 3 mg/kg, BACE1-IN-5 achieves a maximal Aβ reduction of 87%, corresponding to a free brain concentration of 9.5 ng/mL (21 nM). |
Molecular Weight | 461.41 |
Formula | C18H16F5N5O2S |
CAS No. | 2581114-83-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BACE1-IN-5 2581114-83-0 Neuroscience Beta Amyloid BACE BACE1IN5 BACE-1-IN-5 BACE1 IN 5 inhibitor inhibit