Art. -Nr.: HY-173371

BRI-50460

Name: BRI-50460
Brand: MedChemExpress
SKU: HY-173371
Price: 135.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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BRI-50460 is a brain-penetrant selective cPLA₂ inhibitor with an IC₅₀ of 0.88 nM. BRI-50460 inhibits cPLA₂ to modulate downstream inflammatory lipid signaling pathways, attenuating Aβ42 oligomer-induced synaptic loss and tau hyperphosphorylation, thereby exerting effects of modulating neuroinflammation and restoring lipid homeostasis. BRI-50460 can be used in research in the fields of Alzheimer's disease and other neurodegenerative diseases.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.62%
Formel: C₂₁H₁₈N₂O₄S
Molecular Weight:394.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BRI-50460 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

HY-116301
CAY10502

cPLA2α Inhibitor

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

cPLA₂

0.88 nM (IC₅₀)

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

In Vitro

Aβ/Tau/α-Synuclein AggregationInnate ImmunityOthers

Aβ/Tau/α-Synuclein Aggregation

Innate Immunity

BRI-50460 (1 μM; co-incubation for 72 h) attenuates Aβ42O-induced cPLA2α hyperphosphorylation, tau hyperphosphorylation, and protects against synaptic loss in Aβ42O-treated mixed cultures of human iPSC-derived neurons and astrocytes^[1].

Innate Immunity

Aβ/Tau/α-Synuclein Aggregation

BRI-50460 (0.1-1 μM; pretreatment for 30 min + co-incubation for 72 h) significantly reduces Aβ-induced elevation of cPLA2 protein levels and its phosphorylation levels in Aβ42O (HY-P1363A)-treated human iPSC-derived astrocytes (APOE3/3 genotype)^[1].

Others

BRI-50460 (3 h pre-incubation) inhibits cPLA₂-mediated arachidonic acid release in A-23187 (HY-N6687)-stimulated BV2 cells with an IC₅₀ of 0.88 nM; it also inhibits downstream PGE₂ production with an IC₅₀ of 4.1 nM^[1].
BRI-50460 (up to 1 μM) shows no cytotoxicity in HEK293 and HMC3 cells^[1].
BRI-50460 (up to 50 μM; 10-30 min) shows no inhibitory activity against the non-target enzyme iPLA2 in biochemical assays of lysates from cells expressing iPLA2 (demonstrating extremely high cPLA2 selectivity, with a selectivity window of > 100-fold)^[1].

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

Western Blot Analysis^[1]

Cell Line:

human iPSC-derived astrocytes (APOE ε3/ε3)
Concentration:

0.1, 1 μM (BRI-50460); 2.5 μM (Aβ42O)
Incubation Time:

30 min (BRI-50460 pre-incubation); 72 h (Aβ42O)
Result:

Reduced Aβ-related increases in cPLA2 levels and caused a reduction in phosphorylated cPLA2 at 1 μM.

Immunofluorescence^[1]

Cell Line:

human iPSC-derived neuron/astrocyte mixed culture (APOE3/3)
Concentration:

1 μM (BRI-50460); 2.5 μM (Aβ42O)
Incubation Time:

72 h
Result:

Reduced Aβ42O-induced increases in phospho-cPLA2α(Ser505) and phospho-tau (Ser202/Thr205) in human neurons.

Immunofluorescence^[1]

Cell Line:

human iPSC-derived neuron/astrocyte mixed culture (APOE4/4)
Concentration:

1 μM (BRI-50460); 2.5 μM (Aβ42O)
Incubation Time:

72 h
Result:

Protected the cells from Aβ42O-induced reductions of synaptic puncta stained by synapsin and dendritic density (occupied area) stained by CamKIIα and MAP2.

Parmacokinetics

Species	Dose	Route	T_max (Plasma)	T_1/2 (Plasma)	C_max (Brain)	T_max (Brain)	T_1/2 (Brain)	Bioavailability	Brain-to-Plasma Ratio
Mice^[1]	3 mg/kg	s.c.	1 h	2.3 h	2.909 ng/mL	1 h	3.532 h	/	49 %
Mice^[1]	3 mg/kg	p.o.	1 h	4.2 h	2.458 ng/mL	0.5 h	3.954 h	37.9 %	/

In Vivo

BRI-50460 (3 mg/kg; p.o. or s.c.; single dose; 6 h) exhibits favorable pharmacokinetic properties in C57BL/6J mice, including rapid penetration of the blood-brain barrier to enter the central nervous system (brain-to-plasma exposure ratio B/P ratio of over 40%) and long-lasting maintenance of effect^[1].

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

Related Protocols :

Chemical Information

Appearance Solid
Molecular Weight 394.44
Formel C₂₁H₁₈N₂O₄S
Color White to off-white
SMILES

O=C(CC1)NC2=C1C=CC(NS(C3=CC=CC(OC4=CC=CC=C4)=C3)(=O)=O)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (253.52 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

2.5352 mL

12.6762 mL

25.3524 mL

5 mM

0.5070 mL

2.5352 mL

5.0705 mL

10 mM

0.2535 mL

1.2676 mL

2.5352 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.

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)}

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 (6.34 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). 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 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.34 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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]. Sadybekov AV, et al. Development of potent, selective cPLA inhibitors for targeting neuroinflammation in Alzheimer's disease and other neurodegenerative disorders. npj drug discovery. 2026;3(1):2.

[2]. Sadybekov AV, Duro MV, Wang S, Ebright B, Dikeman D, Hugo C, Kerman BE, Ma QL, Nazarova AL, Sadybekov AA, Asante I, Louie SG, Katritch V, Yassine HN. Development of potent, selective cPLA2 inhibitors for targeting neuroinflammation in Alzheimer's disease and other neurodegenerative disorders. NPJ Drug Discov. 2026;3(1):2.

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	2.5352 mL	12.6762 mL	25.3524 mL	63.3810 mL
	5 mM	0.5070 mL	2.5352 mL	5.0705 mL	12.6762 mL
	10 mM	0.2535 mL	1.2676 mL	2.5352 mL	6.3381 mL
	15 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2254 mL
	20 mM	0.1268 mL	0.6338 mL	1.2676 mL	3.1690 mL
	25 mM	0.1014 mL	0.5070 mL	1.0141 mL	2.5352 mL
	30 mM	0.0845 mL	0.4225 mL	0.8451 mL	2.1127 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5845 mL
	50 mM	0.0507 mL	0.2535 mL	0.5070 mL	1.2676 mL
	60 mM	0.0423 mL	0.2113 mL	0.4225 mL	1.0563 mL
	80 mM	0.0317 mL	0.1585 mL	0.3169 mL	0.7923 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

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BRI-50460

Alle Phospholipase Isoform-spezifische Produkte anzeigen