GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

LY2811376 LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more th
In vitro

LY2811376 demonstrates concentration-dependent inhibition of hBACE1 with an IC50 of 239 and 249 nM against a small synthetic peptide or a larger chimeric protein substrate, respectively. LY2811376 treatment yields a concentration-dependent decrease in Aβ secretion in APP-overexpressing HEK293 cells. LY2811376 inhibits Aβ secretion with EC50 of ~100 nM in primary neuronal cultures of PDAPP transgenic mouse.

In vivo

Administration of LY2811376 (10, 30, and 100 mg/kg doses) results in dose-dependent, significant reductions in Aβ, as well as sAPPβ and C99, the proximal cleavage products of APP proteolysis by BACE1 in APP^V717F mouse model of Aβ pathology. After treatment with LY2811376 (5 mg/kg), reductions in Aβ_1-x are observed in plasma, with a maximal 85% reduction observed from 4 to 12 h after dosing in beagle dogs.
Cell Data

cell lines：MV-4-11, MOLM-13, and OCI-AML-3 cell lines

Concentrations：~ 100 μM

Incubation Time：48–72 hours

Powder Purity:≥99%

Specifications

Synonyms

(S)-4-(2, 4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5, 6-dihydro-4H-1, 3-thiazin-2-amine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold i

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of beta-secretase 1

Names and Identifiers

• Isomeric SMILES: C[C@]1(CCSC(=N1)N)C2=C(C=C(C(=C2)C3=CN=CN=C3)F)F
• Molecular Weight: 320.36
• Reaxy-Rn: 45675369
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=45675369&ln=

Associated Targets(Human)

BACE1 Tchem Beta-secretase 1 (14 Activities)

Discover Target: BACE1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BACE2 Tchem Beta-secretase 2 (1 Activities)

Discover Target: BACE2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)