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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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 |
Potent lp-PLA2inhibitor
Synonyms | BCP9000585 | 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 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent lipoprotein-associated phospholipase A2(lp-PLA2) inhibitor (IC50= 5 nM in whole human plasma). |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | LDL-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. |
ALogP | 7 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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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 |
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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 |
CAS Registry No. | 356057-34-6 |
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ChEMBL Ligand | CHEMBL204021 |
PubChem CID | 9939609 |
Wikipedia | Darapladib |
RCSB PDB Ligand | 5HV |
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Solubility | Solvent:DMSO, Max Conc. mg/mL: 66.68, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 66.68, Max Conc. mM: 100 |
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Pictogram(s) | GHS09, GHS05 |
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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. |
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] [10.1021/op500134e] |
2. Wilensky RL, Macphee CH. (2009) Lipoprotein-associated phospholipase A(2) and atherosclerosis.. Curr Opin Lipidol, 20 (5): (415-20). [PMID:19667981] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |
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] [10.1021/op500134e] |