WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319503
CAS#: 412950-08-4
Description: Rilapladib, aslo known as SB-659032 and GTPL7376, is a lipoprotein-associated phospholipase A2 inhibitor.
Hodoodo Cat#: H319503
Name: Rilapladib
CAS#: 412950-08-4
Chemical Formula: C40H38F5N3O3S
Exact Mass: 735.26
Molecular Weight: 735.814
Elemental Analysis: C, 65.29; H, 5.21; F, 12.91; N, 5.71; O, 6.52; S, 4.36
Synonym: SB-659032; SB659032; SB 659032; GTPL7376; GTPL-7376; GTPL 7376; D05728; Rilapladib
IUPAC/Chemical Name: 2-[2-[(2,3-difluorophenyl)methylsulfanyl]-4-oxoquinolin-1-yl]-N-[1-(2-methoxyethyl)piperidin-4-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
InChi Key: NNBGCSGCRSCFEA-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: O=C(N(C1CCN(CCOC)CC1)CC2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)CN4C(SCC5=CC=CC(F)=C5F)=CC(C6=C4C=CC=C6)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 735.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Shaddinger BC, Xu Y, Roger JH, Macphee CH, Handel M, Baidoo CA, Magee M,
Lepore JJ, Sprecher DL. Platelet aggregation unchanged by lipoprotein-associated
phospholipase A₂ inhibition: results from an in vitro study and two randomized
phase I trials. PLoS One. 2014 Jan 27;9(1):e83094. doi:
10.1371/journal.pone.0083094. eCollection 2014. PubMed PMID: 24475026; PubMed
Central PMCID: PMC3903475.
2: Tawakol A, Singh P, Rudd JH, Soffer J, Cai G, Vucic E, Brannan SP, Tarka EA,
Shaddinger BC, Sarov-Blat L, Matthews P, Subramanian S, Farkouh M, Fayad ZA.
Effect of treatment for 12 weeks with rilapladib, a lipoprotein-associated
phospholipase A2 inhibitor, on arterial inflammation as assessed with
18F-fluorodeoxyglucose-positron emission tomography imaging. J Am Coll Cardiol.
2014 Jan 7-14;63(1):86-8. doi: 10.1016/j.jacc.2013.07.050. Epub 2013 Aug 21.
PubMed PMID: 23973698.