(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
CAS: 209984-57-6
Molecular Formula: C26H23F2N3O4
(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 - Names and Identifiers
(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 - Physico-chemical Properties
| Molecular Formula | C26H23F2N3O4 |
| Molar Mass | 479.48 |
| Density | 1.40 |
| Boling Point | 836.0±65.0 °C(Predicted) |
| Solubility | DMSO: soluble5mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 11.79±0.20(Predicted) |
| Storage Condition | -20°C |
| MDL | MFCD09832551 |
| Use | LY-411575 |
| In vitro study | LY-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 study | A 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. |
(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 - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| HS Code | 29337900 |
(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 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.086 ml | 10.428 ml | 20.856 ml |
| 5 mM | 0.417 ml | 2.086 ml | 4.171 ml |
| 10 mM | 0.209 ml | 1.043 ml | 2.086 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.417 ml |
Last Update：2024-01-02 23:10:35
(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 - 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 |
| Target | Value |
| 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
![(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](http://res.chembk.com/assets/images/structure/304476.gif)
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Product Name: LY-411575 Visit Supplier Webpage Request for quotation
CAS: 209984-57-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 209984-57-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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