Products

Enzymes for Research, Diagnostic and Industrial Use

Darapladib

Cat No.
CEI-1308
Description
Darapladib (SB-480848) is a reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2)with IC50 of 0.25 nM.
Product Overview
Plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. Lipoprotein-associated phospholipase A2 (Lp-PLA2) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. Darapladib is a selective inhibitor of Lp-PLA2. Clinical trial: Darapladib produced sustained inhibition of plasma Lp-PLA2 activity in patients receiving intensive atorvastatin therapy. IL-6 and hs-CRP changes after 12 weeks of darapladib 160 mg suggested a possible reduction in inflammatory burden.
CAS No.
356057-34-6
Molecular Weight
666.77
Purity
0.9969
Storage
Store at -20°C
Synonyms
SB-480848; SB480848; SB 480848
Targets
Lp-PLA2
IC50
0.25 nM
Molecular Formula
C36H38F4N4O2S
Chemical Name
N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
Darapladib potently inhibited Lp-PLA2 with an IC50 of 270 pM. A lack of selectivity against other secretory PLA2s postulated to play a role in atherogenesis had been demonstrated. The percentage inhibition achieved when 1 μM darapladib was evaluated against human secretory PLA2s IIA, V and X, was 0, 0 and 8.7%, respectively.
In vivo
Inhibition of lp-PLA2 by darapladib led to attenuation of inflammation in vivo and decreased plaque formation in ApoE-deficient mice, suggesting an anti-atherogenic role during the progression of atherosclerosis.
Download Datasheet:



Inquiry
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: