Description
LY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme.
Product information
CAS Number: 164083-84-5
Molecular Weight: 430.43
Formula: C22H27N2O5P
Chemical Name: (3-{[1-benzyl-3-(carbamoylmethyl)-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid
Smiles: CCC1=C(CC(N)=O)C2=CC(=CC=C2N1CC1C=CC=CC=1)OCCCP(O)(O)=O
InChiKey: OPWQYOUZRHDKBR-UHFFFAOYSA-N
InChi: InChI=1S/C22H27N2O5P/c1-2-20-19(14-22(23)25)18-13-17(29-11-6-12-30(26,27)28)9-10-21(18)24(20)15-16-7-4-3-5-8-16/h3-5,7-10,13H,2,6,11-12,14-15H2,1H3,(H2,23,25)(H2,26,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
LY-311727 (0.1-10 μM) suppresses the contractile responses induced by human non-pancreatic secretory phospholipase A2 (hnps-PLA2), in a concentration related manner. LY-311727 nearly abolishes the hnps-PLA2 responses at 1 μM, while it failed to suppress porcine pancreatic PLA2 concentration response curves at the same concentration. LY-311727 displays 1,500-fold selectivity when assayed against porcine pancreatic s-PLA2.
In Vivo:
LY-311727 (3-30 mg/kg; i.v.) dramatically suppresses the circulating enzyme activity in mice with metallothionein promoter-human secretory PLA2 minigene (Mt-sPLA2) transgenic the intravenous (i.v.) administration.
Products are for research use only. Not for human use.
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