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Darapladib - ≥98%, high purity , LDL-associated phospholipase A2 inhibitor, CAS No.356057-34-6, LDL-associated phospholipase A2 inhibitor

Item Number
D125951
Grouped product items
SKUSizeAvailabilityPrice Qty
D125951-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$127.90
D125951-10mg
10mg
In stock
$206.90
D125951-50mg
50mg
In stock
$672.90
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Potent lp-PLA2inhibitor

View related series
PLA2-G7 Inhibitor

Basic Description

SynonymsBCP9000585 | BDBM50524488 | DARAPLADIB [MI] | 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 | SB 480848 | NCGC00386337
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent lipoprotein-associated phospholipase A2(lp-PLA2) inhibitor (IC50= 5 nM in whole human plasma).
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionLDL-associated phospholipase A2 inhibitor
Note卖完停产，不再备货
Product Description

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

Product Properties

ALogP7

Associated Targets(Human)

PLA2G7 Tchem Platelet-activating factor acetylhydrolase (19 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PLA2G7 Tchem LDL-associated phospholipase A2 (1338 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Homo sapiens (32628 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pla2g7 Platelet-activating factor acetylhydrolase (22 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC 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
INCHI InChI=1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3
InChi Key WDPFJWLDPVQCAJ-UHFFFAOYSA-N
Canonical SMILES CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
Isomeric SMILES CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
PubChem CID 9939609
Molecular Weight 666.77

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

3 results found

Lot NumberCertificate TypeDateItem
A2213306Certificate of AnalysisOct 20, 2023 D125951
A2213347Certificate of AnalysisOct 20, 2023 D125951
B1525028Certificate of AnalysisSep 15, 2022 D125951

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 66.68, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 66.68, Max Conc. mM: 100

Safety and Hazards(GHS)

Pictogram(s) GHS09,   GHS05
Signal Danger
Hazard Statements

H318:Causes serious eye damage

H400:Very toxic to aquatic life

H410:Very toxic to aquatic life with long lasting effects

Precautionary Statements

P273:Avoid release to the environment.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P501:Dispose of contents/container to ...

P391:Collect spillage.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P305+P354+P338:IF IN EYES: Immediately rinse with water for several minutes. Remove contact lenses if present and easy to do. Continue rinsing.

P317:Get emergency medical help.

Related Documents

 SDS

 Specification Sheet

References

1. Mohler 3rd ER, Ballantyne CM, Davidson MH, Hanefeld M, Ruilope LM, Johnson JL, Zalewski A, Darapladib Investigators.  (2008)  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,  51  (17): (1632-41).  [PMID:18436114]
2. Wilensky RL, Macphee CH.  (2009)  Lipoprotein-associated phospholipase A(2) and atherosclerosis..  Curr Opin Lipidol,  20  (5): (415-20).  [PMID:19667981]
3. O'Donoghue ML, Braunwald E, White HD, Serruys P, Steg PG, Hochman J, Maggioni AP, Bode C, Weaver D, Johnson JL et al..  (2011)  Study design and rationale for the Stabilization of pLaques usIng Darapladib-Thrombolysis in Myocardial Infarction (SOLID-TIMI 52) trial in patients after an acute coronary syndrome..  Am Heart J,  162  (4): (613-619.e1).  [PMID:21982651]
4. STABILITY Investigators, White HD, Held C, Stewart R, Tarka E, Brown R, Davies RY, Budaj A, Harrington RA, Steg PG et al..  (2014)  Darapladib for preventing ischemic events in stable coronary heart disease..  N Engl J Med,  370  (18): (1702-11).  [PMID:24678955]
5. O'Donoghue ML, Braunwald E, White HD, Steen DP, Lukas MA, Tarka E, Steg PG, Hochman JS, Bode C, Maggioni AP et al..  (2014)  Effect of darapladib on major coronary events after an acute coronary syndrome: the SOLID-TIMI 52 randomized clinical trial..  JAMA,  312  (10): (1006-15).  [PMID:25173516]
6. Staurenghi G, Ye L, Magee MH, Danis RP, Wurzelmann J, Adamson P, McLaughlin MM, Darapladib DME Study Group.  (2015)  Darapladib, a lipoprotein-associated phospholipase A2 inhibitor, in diabetic macular edema: a 3-month placebo-controlled study..  Ophthalmology,  122  (5): (990-6).  [PMID:25749297]
7. Sofogianni A, Alkagiet S, Tziomalos K.  (2018)  Lipoprotein-associated Phospholipase A2 and Coronary Heart Disease..  Curr Pharm Des,  24  (3): (291-296).  [PMID:29332572]
8. Tian Y, Jia H, Li S, Wu Y, Guo L, Tan G, Li B.  (2017)  The associations of stroke, transient ischemic attack, and/or stroke-related recurrent vascular events with Lipoprotein-associated phospholipase A2: A systematic review and meta-analysis..  Medicine (Baltimore),  96  (51): (e9413).  [PMID:29390564]
9. Tjoelker LW, Wilder C, Eberhardt C, Stafforini DM, Dietsch G, Schimpf B, Hooper S, Le Trong H, Cousens LS, Zimmerman GA et al..  (1995)  Anti-inflammatory properties of a platelet-activating factor acetylhydrolase..  Nature,  374  (6522): (549-53).  [PMID:7700381]

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