[CAS NO. 356057-34-6] Darapladib (SB-480848)

Name: Darapladib (SB-480848)
Brand: Arctom Scientific
SKU: SLK-S7520

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PRODUCTS SPECIFICATIONS [356057-34-6]

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Catalog

SLK-S7520

Brand

Selleck

CAS

356057-34-6

DESCRIPTION [356057-34-6]

Overview

MDL	MFCD18251452
Molecular Weight	666.77
Molecular Formula	C36H38F4N4O2S
SMILES	C(C(N(CC1=CC=C(C=C1)C2=CC=C(C(F)(F)F)C=C2)CCN(CC)CC)=O)N3C4=C(C(=O)N=C3SCC5=CC=C(F)C=C5)CCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.4998 mL	7.4988 mL	14.9977 mL
5 mM	0.3000 mL	1.4998 mL	2.9995 mL
10 mM	0.1500 mL	0.7499 mL	1.4998 mL
50 mM	0.0300 mL	0.1500 mL	0.3000 mL

Description

Darapladib (SB-480848) is a reversible inhibitor with of 0.25 nM. Phase 3.

Targets

Lp-PLA2 ^[1]
(Cell-free assay)

0.25 nM

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.

References

[1] Blackie JA, et al. Bioorg Med Chem Lett. 2003, 13(6), 1067-1070.
[2] Wilensky RL, et al. Nat Med. 2008, 14(10), 1059-1066.
[3] Acharya NK, et al. J Alzheimers Dis. 2013, 35(1), 179-198.

Synonyms

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]-

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

1-[[[N-[2-(Diethylamino)ethyl]-N-[4-[4-(trifluoromethyl)phenyl]benzyl]amino]carbonyl]methyl]-2-(4-fluorobenzylthio)-5,6-trimethylenepyrimidin-4-one

SB 480848

SB 435445

Darapladib