BACE1/2-IN-1

Modify Date: 2024-01-16 12:19:04

BACE1/2-IN-1 structure	Common Name	BACE1/2-IN-1
	CAS Number	2671036-34-1	Molecular Weight	401.57
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₃₁N₅OS	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of BACE1/2-IN-1

BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].

Name	BACE1/2-IN-1

Description	BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Beta-secretase Research Areas >> Neurological Disease
Target	IC50: 0.0053 μM (BACE2), 0.01 μM (BACE1), 160 μM (Cathepsin D)[1]
In Vitro	BACE1/2-IN-1 (compound 34) demonstrates slight selectivity for BACE2 and retained >3000 fold selectivity against Cathepsin D[1].
In Vivo	BACE1/2-IN-1 (compound 34) (PDAPP (V717F) transgenic mice, 0-100 mg/kg, Subcutaneous injection, once) shows significant reduction in PDAPP mouse cortex Aβ at 100 mg/kg (40%), and 30 mg/kg (24%), but not at 10 mg/kg (12%NS)[1].
References	[1]. Winneroski LL, et al. Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints. Bioorg Med Chem. 2020 Jan 1;28(1):115194.

Molecular Formula	C₂₁H₃₁N₅OS
Molecular Weight	401.57

BACE1/2-IN-1

Use of BACE1/2-IN-1

Names

BACE1/2-IN-1 Biological Activity

Chemical & Physical Properties