DARAPLADIB

Description In vitro In vivo

Product Name: DARAPLADIB
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
Formula Weight: 666.77
MOL File: 356057-34-6.mol

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DARAPLADIB Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H318Causes serious eye damage

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P310Immediately call a POISON CENTER or doctor/physician.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16429
Product name: Darapladib
Purity: ≥98%
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 16429
Product name: Darapladib
Purity: ≥98%
Packaging: 5mg
Price: $168
Updated: 2024/03/01

Cayman Chemical

Product number: 16429
Product name: Darapladib
Purity: ≥98%
Packaging: 10mg
Price: $310
Updated: 2024/03/01

Cayman Chemical

Product number: 16429
Product name: Darapladib
Purity: ≥98%
Packaging: 25mg
Price: $699
Updated: 2024/03/01

TRC

Product number: D194920
Product name: Darapladib
Packaging: 1mg
Price: $50
Updated: 2021/12/16

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DARAPLADIB Chemical Properties,Usage,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

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DARAPLADIB Suppliers

China 84 India 2 United Kingdom 3 United States 17 Global 106

Shanghai Jiyi Biological Technology Co., LTD

Tel: 021-54135696 18516235431
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Shanghai Boyle Chemical Co., Ltd.

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Chembest Research Laboratories Limited

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Nanjing Vital Chemical Co., Ltd.

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Shanghai Sphchem Co., Ltd.

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Dalian Meilun Biotech Co., Ltd.

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Haoyuan Chemexpress Co., Ltd.

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Shanghai Aladdin Bio-Chem Technology Co.,LTD

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China Nobel Chem Co., Limited

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EnliPharma Technology Co., Ltd

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356057-34-6, DARAPLADIBRelated Search:

N-Ethylacetamide 2-Aminoethyl(ethyl)amine N-Ethyl-3-methylaniline N-ethyl-pyrrolidone Necrostatin-1 Saracatinib Dabrafenib Afatinib Fulvestrant Z-VAD-FMK

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

CS-1426

SB-480848; SB480848; SB 480848

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]-

DARAPLADIB USP/EP/BP

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