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
- Molecular Weight:
- 666.77
- MDL Number:
- MFCD18251452
- MOL File:
- 356057-34-6.mol
- MSDS File:
- SDS
| 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) |
| FDA UNII | UI1U1MYH09 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   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 |
|
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 |
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | +86-29-87569265 +86-18612256290 | 1056@dideu.com | China | 3581 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aceschem Inc. | +1-817863-6948 +1-（817）863-6948 | sales@aceschem.com | United States | 19639 | 58 |
View Lastest Price from DARAPLADIB manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2021-07-20 | Darapladib
356057-34-6
|
US $0.00-0.00 / KG | 5mg | 99% | 2000tons | Shaanxi Dideu Medichem Co. Ltd |
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- Darapladib
356057-34-6
- US $0.00-0.00 / KG
- 99%
- Shaanxi Dideu Medichem Co. Ltd