LY2811376 - Moligand™, 10mM in DMSO , Inhibitor of beta-secretase 1, CAS No.1194044-20-6, Inhibitor of beta-secretase 1

CAS: 1194044-20-6 Cat. No.: L409213 Summenformel: C₁₅H₁₄F₂N₄S Molekulargewicht: 320.36

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

Übersicht

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

Synonyme

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

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

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

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of beta-secretase 1

Namen und Kennungen

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

Zugehörige Ziele (menschlich)

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)

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1194044-20-6, the molecular formula is C15H14F2N4S, and the molecular weight is 320.36 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.