RILAPLADIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C40H38F5N3O3S
Molecular Weight	735.805
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COCCN1CCC(CC1)N(CC2=CC=C(C=C2)C3=CC=C(C=C3)C(F)(F)F)C(=O)CN4C(SCC5=C(F)C(F)=CC=C5)=CC(=O)C6=C4C=CC=C6

InChI

InChIKey=NNBGCSGCRSCFEA-UHFFFAOYSA-N

InChI=1S/C40H38F5N3O3S/c1-51-22-21-46-19-17-32(18-20-46)47(24-27-9-11-28(12-10-27)29-13-15-31(16-14-29)40(43,44)45)37(50)25-48-35-8-3-2-6-33(35)36(49)23-38(48)52-26-30-5-4-7-34(41)39(30)42/h2-16,23,32H,17-22,24-26H2,1H3

HIDE SMILES / InChI

Molecular Formula	C40H38F5N3O3S
Molecular Weight	735.805
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29854933 | https://clinicaltrials.gov/ct2/show/results/NCT01428453 | https://www.ncbi.nlm.nih.gov/pubmed/23973698 | https://www.drugbank.ca/drugs/DB05119

Rilapladib (SB659032) is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Inhibition of Lp-PLA2 can reduce peripheral measures of inflammation. Rilapladib has been evaluated for treatment in Alzheimer’s disease and atherosclerosis. Initial results from clinical trials in Alzheimer patients suggests that oral administration of rilapladib may slow down the progression of Alzheimer’s disease. Initial evidence has also been found that inhibition of Lp-PLA2 may attenuate intimal macrophage accumulation and consequently stabilize atherosclerotic plaque.

Originator

Approval Year

PubMed

Title	Date	PubMed
Lipoprotein-associated phospholipase A(2) and atherosclerosis.	2009 Oct	19667981
Plasma lipoprotein-associated phospholipase A2 activity in Alzheimer's disease, amnestic mild cognitive impairment, and cognitively healthy elderly subjects: a cross-sectional study.	2012	23217243
Lipoprotein-associated phospholipase A2 and risk of dementia in the Cardiovascular Health Study.	2014 Aug	24929287

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:31:10 GMT 2023` Edited by `admin` on `Fri Dec 15 16:31:10 GMT 2023`
Record UNII	O14CWE893Z
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

RILAPLADIB

Official Name

English

SB-659032

Code

English

RILAPLADIB [USAN]

Common Name

English

rilapladib [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29703