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AZD2716
- Optical Purity: 98% e.e.
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C24H23NO3
- MW: 373.44
Description
AZD2716 is a potent secreted phospholipase A2 (sPLA2) inhibitor with IC50 values of 10, 40, and 400 nM for sPLA2-IIa, -V, and -X isoforms, respectively. It exhibits excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and a minimized safety risk profile. When incubated with HepG2 cells, AZD2716 effectively inhibited cellular sPLA2 activity and modulates sPLA₂-dependent biological signaling.
sPLA2 pharmacology plays a critical role in disease-relevant cellular and translational research models; AZD2716 serves as a valuable tool for mechanistic and pathway-focused studies of sPLA2 across biochemical, cellular and disease-model assays.
Key Features
- Multi-Isoform sPLA₂ Inhibitor: Targets sPLA₂-IIa (10 nM), -V (40 nM), and -X (400 nM).
- Favorable Preclinical PK: Shows excellent pharmacokinetic profiles with low safety risks.
- Cellular Signaling Modulator: Blocks cell-based sPLA₂ activity and downstream pathways.
- Versatile Research Tool: Supports sPLA₂ pathway studies
Applications
- sPLA2 pharmacology and target-validation studies
- Cardiovascular Disease Research
- Lipid Cascade Profiling
- Translational Vascular System Research
More Information
| Parent CAS No. | 1845753-81-2 |
|---|---|
| Chemical Name | (R)-3-(5'-Benzyl-2'-carbamoylbiphenyl-3-yl)-2-methylpropanoic acid |
| SMILES | C1C=C(CC2C=CC(C(N)=O)=C(C3C=CC=C(C[C@@H](C)C(=O)O)C=3)C=2)C=CC=1 |&1:18,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H23NO3/c1-16(24(27)28)12-18-8-5-9-20(14-18)22-15-19(10-11-21(22)23(25)26)13-17-6-3-2-4-7-17/h2-11,14-16H,12-13H2,1H3,(H2,25,26)(H,27,28)/t16-/m1/s1 |
| InChiKey | PXRCDPVYRPKGGI-MRXNPFEDSA-N |
| CID | 129909859 |
| Short Description | sPLA2 inhibitor |
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