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LY411575

LY-411575

CAS: 209984-57-6

Molecular Formula: C26H23F2N3O4

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LY411575 - Names and Identifiers

Name LY-411575
Synonyms LY411575
LY-411575
LSN-411575
(S)-2-(2-(3,5-difluorophenyl)acetaMido)-N-((S)-5-Methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanaMide
N2-[(2S)-2-(3,5-Difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide
(aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide
Benzeneacetamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-α-hydroxy-, (αS)-
(aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide LY 411575
LY 411575 (aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide
CAS 209984-57-6
InChIKey ULSSJYNJIZWPSB-CVRXJBIPSA-N

LY411575 - Physico-chemical Properties

Molecular FormulaC26H23F2N3O4
Molar Mass479.48
Density1.40
Boling Point836.0±65.0 °C(Predicted)
Solubility DMSO: soluble5mg/mL, clear
Appearancepowder
Colorwhite to beige
pKa11.79±0.20(Predicted)
Storage Condition-20°C
MDLMFCD09832551
UseLY-411575
In vitro studyLY-411575 inhibits gamma-secretion, which can be assessed by substrate amyloid precursor protein (APP) and Notch S3 cleavage. In primary and immortalized KS cells, LY-411575 blocked Notch activation, leading to apoptosis.
In vivo studyA LY-411575 dose-dependent reduction in brain and plasma Aβ40 and Aβ42 was achieved at an oral dose of 10 mg/kg. In young transgenic CRND8 mice, LY-411575 reduced cortical Aβ40(ED50 ≈ 0.6 mg/kg), and at higher doses (>3 mg/kg), significant thymic atrophy and intestinal goblet cell hyperplasia. The therapeutic window was similar for both oral and subcutaneous administration in young and old CRND8 mice. Thymic and intestinal side effects are reversible after a 2-week washout period. Treatment with 1 mg/kg LY411575 for 3 weeks reduced cortical Aβ40 by 69% without inducing an intestinal effect, although a previously unreported change in coat color would be observed.

LY411575 - Risk and Safety

Safety Description24/25 - Avoid contact with skin and eyes.
WGK Germany3
HS Code29337900

LY411575 - Preparation solution concentration reference

 1mg5mg10mg
1 mM2.086 ml10.428 ml20.856 ml
5 mM0.417 ml2.086 ml4.171 ml
10 mM0.209 ml1.043 ml2.086 ml
5 mM0.042 ml0.209 ml0.417 ml
Last Update：2024-01-02 23:10:35

LY411575 - Reference Information

biological activity LY411575 is an effective γ-secretase inhibitor. IC50 is 0.078 nM/0.082 nM (based on membrane/cell) in HEK293 cells expressing APP or NΔE, which also inhibits Notch division and IC50 is 0.39 nM. LY411575 can induce apoptosis.
target TargetValue gamma secretase (membrane-based) (hek293 cells expressing either app or nΔ e) 0.078 nmγ secretase (hek293 cells expressing either app or nΔ e) 0.082 nmnotch S3 cleavage (hek293 cells expressing either app or nΔ e) 0.39 nm
TargetValue
γ secretase (membrane-based) (HEK293 cells expressing either APP or NΔE) 0.078 nM
γ secretase (cell-based) (HEK293 cells expressing either APP or NΔE) 0.082 nM
Notch S3 cleavage (HEK293 cells expressing either APP or NΔE) 0.39 nM
in vitro study LY-411575 inhibit γ-secretion, which can be evaluated by substrate amyloid precursor protein (APP) and Notch S3 cleavage. In primary and immortalized KS cells, LY-411575 blocked Notch activation, resulting in apoptosis.
in vivo study 10 mg/kg oral dose LY-411575 dose-dependent reduction of brain and plasma Aβ40 and Aβ42. In young (preplaque) transgenic CRND8 mice, the cortical layer Aβ40(ED50 ≈ 0.6 mg/kg) was LY-411575 reduced, and at higher doses (>3 mg/kg), significant thymus atrophy and intestinal goblet cell proliferation were produced. In young and old CRND8 mice, oral and subcutaneous administration, the therapeutic window is similar. Thymus and intestinal side effects are reversible after a 2-week clearance period. Treatment with 1 mg/kg LY411575 for 3 weeks reduced 69% cortical Aβ40 without inducing intestinal effects, although previously unreported changes in coat color would be observed.
Last Update：2024-04-10 22:29:15
LY411575
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Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: LY-411575 Request for quotation
CAS: 209984-57-6
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: 609-228-6898
Email: sales@medchemexpress.com
　　　　 tech@medchemexpress.com
Mobile: 609-228-6898
BOC Sciences
Spot supply
Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
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