Art. -Nr.: HY-16632

ELND 006

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ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease.

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Reinheit: 99.7%
CAS. Nr.: 1333990-84-3
Formel: C₂₀H₁₄F₅N₃O₂S
Molecular Weight:455.40

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ELND 006 Chemical Structure

CAS. Nr.: 1333990-84-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	ED₅₀	1.1 nM Compound: 30, ELND006	Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA	[PMID: 23713656]
CHO	ED₅₀	86 nM Compound: 30, ELND006	Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay	[PMID: 23713656]
CHO	IC₅₀	82 nM Compound: ELND006	Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay	[PMID: 23312944]
HEK293	ED₅₀	1.1 nM Compound: ELND006	Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis	[PMID: 23312944]
IMR-32	IC₅₀	0.34 nM Compound: ELND006	Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA	[PMID: 23312944]
IMR-32	IC₅₀	5.3 nM Compound: ELND006	Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA	[PMID: 23312944]

Chemical Information

CAS. Nr. 1333990-84-3
Appearance Solid
Molecular Weight 455.40
Formel C₂₀H₁₄F₅N₃O₂S
Color White to off-white
SMILES

O=S(N1[C@H](C2CC2)C3=C(NN=C3)C4=C1C=C(F)C(F)=C4)(C5=CC=C(C(F)(F)F)C=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (109.79 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1959 mL

10.9794 mL

21.9587 mL

5 mM

0.4392 mL

2.1959 mL

4.3917 mL

10 mM

0.2196 mL

1.0979 mL

2.1959 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Discovery of (R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1959 mL	10.9794 mL	21.9587 mL	54.8968 mL
	5 mM	0.4392 mL	2.1959 mL	4.3917 mL	10.9794 mL
	10 mM	0.2196 mL	1.0979 mL	2.1959 mL	5.4897 mL
	15 mM	0.1464 mL	0.7320 mL	1.4639 mL	3.6598 mL
	20 mM	0.1098 mL	0.5490 mL	1.0979 mL	2.7448 mL
	25 mM	0.0878 mL	0.4392 mL	0.8783 mL	2.1959 mL
	30 mM	0.0732 mL	0.3660 mL	0.7320 mL	1.8299 mL
	40 mM	0.0549 mL	0.2745 mL	0.5490 mL	1.3724 mL
	50 mM	0.0439 mL	0.2196 mL	0.4392 mL	1.0979 mL
	60 mM	0.0366 mL	0.1830 mL	0.3660 mL	0.9149 mL
	80 mM	0.0274 mL	0.1372 mL	0.2745 mL	0.6862 mL
	100 mM	0.0220 mL	0.1098 mL	0.2196 mL	0.5490 mL

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ELND 006

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ELND 006

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ELND 006 Related Classifications

Art. -Nr.: HY-16632