ELND 006

Cat. No.: HY-16632 Purity: 99.7%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

ELND 006 Chemical Structure

CAS No. : 1333990-84-3

Size	Price	Stock	Quantity
5 mg	USD 147	In-stock	Estimated Time of Arrival: December 31
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50 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

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	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]
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]
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]

Molecular Weight

455.40

Formula

C₂₀H₁₄F₅N₃O₂S

CAS No.

1333990-84-3

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.7%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (252 KB)

Handling Instructions (2659 KB)

References

[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

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

ELND 006 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ELND 0061333990-84-3ELND006ELND-006γ-secretaseAmyloid-βGamma secretaseβ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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ELND 006

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