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BACE1-IN-5
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Catalog No. T10453Cas No. 2581114-83-0
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].
BACE1-IN-5
😃Good
Catalog No. T10453Cas No. 2581114-83-0
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 | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 10-14 weeks | |
| 50 mg | $1,980 | 10-14 weeks | |
| 100 mg | $2,500 | 10-14 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Relative Density. | 1.31g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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