country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-106253

Copy Link Print Information

Efipladib

Efipladib is a potent, selective and orally active cPLA₂α inhibitor with an IC₅₀ of 0.04 μM and a K_d of 0.067 μM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 381683-94-9
Formel: C₄₀H₃₅Cl₃N₂O₄S
Molecular Weight:746.14

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

Efipladib Chemical Structure

CAS. Nr.: 381683-94-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Efipladib is a potent, selective and orally active cPLA₂α inhibitor with an IC₅₀ of 0.04 μM and a K_d of 0.067 μM^[1].

IC₅₀ & Target^[1]

cPLA2α

0.04 μM (IC₅₀)

cPLA2α

0.067 μM (Ki)

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MC9	IC₅₀	0.02 μM Compound: 111	Inhibition of LTB4 production in mouse MC9 cells Inhibition of LTB4 production in mouse MC9 cells	[PMID: 18498150]
MC9	IC₅₀	0.02 μM Compound: 111	Inhibition of PGF2alpha production in mouse MC9 cells Inhibition of PGF2alpha production in mouse MC9 cells	[PMID: 18498150]
MC9	IC₅₀	0.9 μM Compound: 111	Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells	[PMID: 18498150]
U-937	IC₅₀	0.00054 μM Compound: 1	Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting	[PMID: 25102418]
U-937	IC₅₀	0.54 nM Compound: 1	Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting	[PMID: 25102418]

In Vitro

Efipladib (10-25 μM; 24-72 h) increases COX-1 and PGE2 levels in PC3 and LNCaP cells^[3].

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

Western Blot Analysis^[3]

Cell Line:

PC3 and LNCaP cells
Concentration:

10, 15, 20 and 25 μM
Incubation Time:

72 h
Result:

Significantly decreased cPLA2α activity. Increased COX-1 protein levels. Increased COX-2 protein levels in PC3 cells.

In Vivo

Efipladib (100 mg/kg; p.o.; BID for 31 days) reverses the severity in mouse collagen-induced arthritis (CIA) model^[1].
Efipladib (100 mg/kg; p.o.; once) significantly inhibits the nociceptive response 1 h after administration in the rat Complete Freund’s Adjuvant (CFA) nociception model^[2].
Efipladib is unable to cross the BBB to gain access to the central compartment^[2].
Efipladib (100 nM; IT; 5 μL) reduces PGE2 levels in the cerebrospinal fluid in rats^[2].

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

Animal Model:

Mouse collagen-induced arthritis (CIA) model^[1]
Dosage:

100 mg/kg
Administration:

PO, BID for 31 days
Result:

Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group.

Animal Model:

Male Sprague-Dawley rats^[2]
Dosage:

100 nM in 5 μL of 100% DMSO/rat
Administration:

Intrathecal administration
Result:

Reduced PGE2 levels in the cerebrospinal fluid (CSF) by 45-60%, yet there was no effect on the nociceptive response.

Chemical Information

CAS. Nr. 381683-94-9
Molecular Weight 746.14
Formel C₄₀H₃₅Cl₃N₂O₄S
SMILES

ClC1=C(Cl)C=CC(CS(NCCC2=C(CCCC3=CC=C(C(O)=O)C=C3)C4=CC(Cl)=CC=C4N2C(C5=CC=CC=C5)C6=CC=CC=C6)(=O)=O)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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]. McKew J C, et al. Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3, 4-dichlorobenzyl) sulfonyl] amino} ethyl)-1-(diphenylmethyl)-1 H-indol-3-yl] propyl} benzoic Acid, Efipladib. Journal of medicinal chemistry, 2008, 51(12): 3388-3413.

[2]. Nickerson-Nutter CL, et al. The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid. Neuropharmacology. 2011 Mar;60(4):633-41. [Content Brief]

[3]. Niknami M, et al. Decrease in expression or activity of cytosolic phospholipase A2alpha increases cyclooxygenase-1 action: A cross-talk between key enzymes in arachidonic acid pathway in prostate cancer cells. Biochim Biophys Acta. 2010 Jul;1801(7):731-7. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Efipladib

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Efipladib Related Classifications

HY-106253 Related Classifications