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
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
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..…
N-Bromosuccinimide Price
- Product number
- 16429
- Product name
- Darapladib
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 16429
- Product name
- Darapladib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $168
- Updated
- 2024/03/01
- Product number
- 16429
- Product name
- Darapladib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $310
- Updated
- 2024/03/01
- Product number
- 16429
- Product name
- Darapladib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $699
- Updated
- 2024/03/01
- Product number
- D194920
- Product name
- Darapladib
- Packaging
- 1mg
- Price
- $50
- Updated
- 2021/12/16
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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