Referencia número: HY-10133

β-Secretase Inhibitor IV

Name: β-Secretase Inhibitor IV
Brand: MedChemExpress
SKU: HY-10133
Price: 240.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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Based on 1 Customer Validation

β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC₅₀s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.19%
No. CAS: 797035-11-1
Fòrmula: C₃₁H₃₈N₄O₅S
Peso molecular:578.72

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

β-Secretase Inhibitor IV Chemical Structure

No. CAS: 797035-11-1

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC₅₀s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.

IC₅₀ & Target

IC50: 15.3±0.6 nM (BACE-1), 230±26 nM (BACE-2), 7620±210 nM (Cathepsin D)^[1]

Ver todos los productos específicos de isoformas Beta-secretase :

BACE1
BACE2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.078 μM Compound: 24	Inhibition of memapsin 2 expressed in CHO cells Inhibition of memapsin 2 expressed in CHO cells	[PMID: 17432843]
CHO	IC₅₀	4.5 x 10^-8 M Compound: IV	Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique	[PMID: 22225636]
CHO	IC₅₀	4.5 x 10^-2 μM Compound: IV	Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique	[PMID: 22225636]
HEK293	IC₅₀	0.25 μM Compound: 2	Inhibition of BACE1 in human HEK293 cells transfected with pCDNA-neo-SEAP-APP assessed as secreted alkaline phosphatase after cleavage of beta-site of APP by fluorescence assay Inhibition of BACE1 in human HEK293 cells transfected with pCDNA-neo-SEAP-APP assessed as secreted alkaline phosphatase after cleavage of beta-site of APP by fluorescence assay	[PMID: 20303626]
HEK-293T	IC₅₀	29 nM Compound: 2	Inhibition of human BACE1 in HEK293T cells transfected with APP695 after 20 to 24 hrs by Western blot analysis Inhibition of human BACE1 in HEK293T cells transfected with APP695 after 20 to 24 hrs by Western blot analysis	[PMID: 20303626]
HEK-293T	EC₅₀	43 nM Compound: IV	Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site assessed as amyloid EV40 secretion Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site assessed as amyloid EV40 secretion	[PMID: 22225636]
HEK-293T	IC₅₀	29 nM Compound: IV	Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site by sAPP_NF cell based assay Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site by sAPP_NF cell based assay	[PMID: 22225636]
N2a	IC₅₀	0.36 μM Compound: IV	Inhibition of beta amyloid 42 secretion in mouse N2a cells Inhibition of beta amyloid 42 secretion in mouse N2a cells	[PMID: 16821787]

In Vitro

In the cell culture assay, β-Secretase Inhibitor IV (Compound 2) inhibits the production of Aβ peptides with an EC₅₀ of 43 nM. β-Secretase Inhibitor IV potently suppresses the secretion of sAPP_{_NF} and EV40 from HEK293T cells with an IC₅₀ near 30 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 797035-11-1
Appearance Solid
Peso molecular 578.72
Fòrmula C₃₁H₃₈N₄O₅S
Color White to light yellow
SMILES

O=S(N(C)C1=CC(C(N[C@@H](CC2=CC=CC=C2)[C@H](O)CNC3CC3)=O)=CC(C(N[C@H](C)C4=CC=CC=C4)=O)=C1)(C)=O
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (172.80 mM; Need ultrasonic; 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

1.7280 mL

8.6398 mL

17.2795 mL

5 mM

0.3456 mL

1.7280 mL

3.4559 mL

10 mM

0.1728 mL

0.8640 mL

1.7280 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.32 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Pietrak BL, et al. Biochemical and cell-based assays for characterization of BACE-1 inhibitors. Anal Biochem. 2005 Jul 1;342(1):144-51. [Content Brief]

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7280 mL	8.6398 mL	17.2795 mL	43.1988 mL
	5 mM	0.3456 mL	1.7280 mL	3.4559 mL	8.6398 mL
	10 mM	0.1728 mL	0.8640 mL	1.7280 mL	4.3199 mL
	15 mM	0.1152 mL	0.5760 mL	1.1520 mL	2.8799 mL
	20 mM	0.0864 mL	0.4320 mL	0.8640 mL	2.1599 mL
	25 mM	0.0691 mL	0.3456 mL	0.6912 mL	1.7280 mL
	30 mM	0.0576 mL	0.2880 mL	0.5760 mL	1.4400 mL
	40 mM	0.0432 mL	0.2160 mL	0.4320 mL	1.0800 mL
	50 mM	0.0346 mL	0.1728 mL	0.3456 mL	0.8640 mL
	60 mM	0.0288 mL	0.1440 mL	0.2880 mL	0.7200 mL
	80 mM	0.0216 mL	0.1080 mL	0.2160 mL	0.5400 mL
	100 mM	0.0173 mL	0.0864 mL	0.1728 mL	0.4320 mL

Bioz

Keywords

β-Secretase Inhibitor IV

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β-Secretase Inhibitor IV

Ver todos los productos específicos de isoformas Beta-secretase

Actividad biológica

Descripciòn

IC50 & Target

Cellular Effect

In Vitro

Chemical Information

Solvente y solubilidad

In Vitro:

In Vivo:

In Vivo Dissolution Calculator

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table