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BACE1-IN-5

Catalog No. T10453 CAS T10453

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC 50 of 9.1 nM. BACE1-IN-5 also inhibits cellular amyloid-β (Aβ) with an IC 50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry to improve hERG inhibition and P-gp efflux [1].

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BACE1-IN-5, CAS T10453

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC 50 of 9.1 nM. BACE1-IN-5 also inhibits cellular amyloid-β (Aβ) with an IC 50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry to improve hERG inhibition and P-gp efflux [1].
Targets&IC50	cellular amyloid-β:0.82 nM , BACE1:9.1 nM
In vivo	BACE1-IN-5 (Compound 15; 1-3 mg/kg; oral administration; for 2-6 hours; male ICR mice) treatment causes a significant and dose-dependent decrease of total Aβ, reduces total Aβ by 76% (4 hours) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. BACE1-IN-5 demonstrats a K p,uu value of 1.3 at 1 mg/kg (4 hours time point). At 3 mg/kg, a maximum Aβ reduction of 87% is achieved at a free brain concentration of 9.5 ng/mL (21 nM) [1]. Animal Model: Male ICR mice [1] Dosage: 1 mg/kg, 3 mg/kg Administration: Oral administration; for 2 hours, 4 hours, and 6 hours Result: A significant and dose-dependent decrease of total Aβ was seen, reduced total Aβ by 76% (4 h) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. Demonstrats a K p,uu value close to 1 (K p,uu of 1.3) at 1 mg/kg (4 h time point). At 3 mg/kg, a maximum Aβ reduction of 87% was achieved at a free brain concentration of 9.5 ng/mL (21 nM).

Molecular Weight	461.41
Formula	C18H16F5N5O2S
CAS No.	T10453

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

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( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Kusakabe KI, et al. Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central Aβ Reduction and Minimal Covalent Binding Burden. ChemMedChem. 2019 Oct 27.

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Keywords

BACE1-IN-5 T10453 神经科学 Beta Amyloid BACE BACE1IN5 BACE-1-IN-5 BACE1 IN 5 Inhibitor inhibitor inhibit

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