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DARAPLADIB

DARAPLADIB Structure
DARAPLADIB structure
CAS No.
356057-34-6
Chemical Name:
DARAPLADIB
Synonyms
CS-1426;SB 480848;SB 435445;Darapladib API;DARAPLADIB USP/EP/BP;Darapladib(SB-480848);DARAPLADIB;SB-480848;SB480848;SB-480848; SB480848; SB 480848;Phospholipase,SB 480848,SB480848,inhibit,Darapladib,Inhibitor;N-[2-(Diethylamino)ethyl]-N-[4'-(trifluoromethyl)-1,1'-biphenyl-4-ylmethyl]-2-[2-(4-fluorobenz
CBNumber:
CB21011731
Molecular Formula:
C36H38F4N4O2S
Molecular Weight:
666.77
MDL Number:
MFCD18251452
MOL File:
356057-34-6.mol
MSDS File:
SDS
Last updated:2024-11-19 20:33:22
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DARAPLADIB Properties

Boiling point 741.0±70.0 °C(Predicted)
Density 1.25
storage temp. Inert atmosphere,Store in freezer, under -20°C
solubility ≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH
form solid
pka 9.03±0.10(Predicted)
color White to off-white
FDA UNII UI1U1MYH09

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS09,GHS05
Signal word  Danger
Hazard statements  H318-H410-H400
Precautionary statements  P273-P391-P501-P273-P391-P501-P280-P305+P351+P338-P310
NFPA 704
0
3 0

DARAPLADIB price More Price(26)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 16429 Darapladib ≥98% 356057-34-6 1mg $49 2024-03-01 Buy
Cayman Chemical 16429 Darapladib ≥98% 356057-34-6 5mg $168 2024-03-01 Buy
Cayman Chemical 16429 Darapladib ≥98% 356057-34-6 10mg $310 2024-03-01 Buy
Cayman Chemical 16429 Darapladib ≥98% 356057-34-6 25mg $699 2024-03-01 Buy
TRC D194920 Darapladib 356057-34-6 1mg $50 2021-12-16 Buy
Product number Packaging Price Buy
16429 1mg $49 Buy
16429 5mg $168 Buy
16429 10mg $310 Buy
16429 25mg $699 Buy
D194920 1mg $50 Buy

DARAPLADIB Chemical Properties,Uses,Production

Description

Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

In vitro

During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM.

In vivo

In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons.

Uses

Treatment of atherosclerosis.

Uses

Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor.

Biological Activity

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.

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 [1].

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 [2].

target

Lp-PLA2

storage

Store at -20°C

References

[1] bui qt, wilensky rl. darapladib. expert opin investig drugs. 2010;19(1):161-8.
[2] wang wy, zhang j, wu wy, li j, ma yl, chen wh, yan h, wang k, xu ww, shen jh, wang yp. inhibition of lipoprotein-associated phospholipase a2 ameliorates inflammation and decreases atherosclerotic plaque formation in apoe-deficient mice. plos one. 2011;6(8):e23425.
[3] mohler er 3rd, ballantyne cm, davidson mh, hanefeld m, ruilope lm, johnson jl, zalewski a; darapladib investigators. the effect of darapladib on plasma lipoprotein-associated phospholipase a2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. j am coll cardiol. 2008;51(17):1632-41.

DARAPLADIB Preparation Products And Raw materials

Raw materials

Preparation Products

DARAPLADIB Suppliers

Global( 107)Suppliers
Supplier Tel Email Country ProdList Advantage
Biochempartner 		0086-13720134139 candy@biochempartner.com CHINA 965 58
Hubei Jusheng Technology Co.,Ltd. 		18871490254 linda@hubeijusheng.com CHINA 28172 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 49374 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32161 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 22787 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
Hangzhou MolCore BioPharmatech Co.,Ltd. 		+86-057181025280; +8617767106207 sales@molcore.com China 49734 58
TargetMol Chemicals Inc. 		support@targetmol.com United States 38631 58
Aceschem Inc. 		+1-817863-6948 +1-（817）863-6948 sales@aceschem.com United States 19632 58
Supplier Advantage
Biochempartner 		58
Hubei Jusheng Technology Co.,Ltd. 		58
BOC Sciences 		58
CONIER CHEM AND PHARMA LIMITED 		58
TargetMol Chemicals Inc. 		58
Dideu Industries Group Limited 		58
InvivoChem 		58
Hangzhou MolCore BioPharmatech Co.,Ltd. 		58
TargetMol Chemicals Inc. 		58
Aceschem Inc. 		58

View Lastest Price from DARAPLADIB manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Darapladib pictures 2024-11-19 Darapladib
356057-34-6
 US $44.00-97.00 / mg 99.85% 10g TargetMol Chemicals Inc.
  • Darapladib pictures
  • Darapladib
    356057-34-6
  • US $44.00-97.00 / mg
  • 99.85%
  • TargetMol Chemicals Inc.

DARAPLADIB Spectrum

DARAPLADIB(356057-34-6)1HNMR

356057-34-6(DARAPLADIB)Related Search:

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1of2

N-[2-(Diethylamino)ethyl]-N-[4'-(trifluoromethyl)-1,1'-biphenyl-4-ylmethyl]-2-[2-(4-fluorobenzylthio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl]acetamide SB 435445 SB 480848 Darapladib API Darapladib(SB-480848) N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-1H-Cyclopentapyrimidine-1-acetamide N-(2-(Diethylamino)ethyl)-2-(2-((4-fluorobenzyl)thio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)-N-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)acetamide DARAPLADIB;SB-480848;SB480848 N-[2-(Diethylamino)ethyl]-N-[4'-(trifluoromethyl)-1,1'-biphenyl-4-ylmethyl]-2-[2-(4-fluorobenz DARAPLADIB USP/EP/BP 1H-Cyclopentapyrimidine-1-acetamide, N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]- SB-480848; SB480848; SB 480848 CS-1426 Phospholipase,SB 480848,SB480848,inhibit,Darapladib,Inhibitor N-(2-(Diethylamino)ethyl)-2-(2-((4-fluorobenzyl)thio)-4-oxo-4,5,6,7-tetrahydro-1H-cyclopenta[d]pyrimidin-1-yl)-N-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)acetamide 356057-34-6 C36H38F4N4O2S Inhibitors