1845753-81-2
Chemical Structure
AZD2716
- CAS No.: 1845753-81-2
- Formula:C24H23NO3
- Molecular Weight:373.44
IUPAC Name: (R)-3-(5'-benzyl-2'-carbamoyl-[1,1'-biphenyl]-3-yl)-2-methylpropanoic acid
InChIKey: PXRCDPVYRPKGGI-MRXNPFEDSA-N
SMILES: NC(C1=C(C2=CC(C[C@@H](C)C(O)=O)=CC=C2)C=C(C=C1)CC3=CC=CC=C3)=O
Biological Activity: AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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AZD2716 | 99.9% | AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming. | ||||||||||||||||||||
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- [1]. Silverman JE. In This Issue, Volume 7, Issue 10. [Content Brief]
- [2]. Salvador GHM, et al. Structural and pharmacological analysis of a PLA2-like toxin in complex with the sPLA2 inhibitor AZD2716: Comparisons to varespladib. Biochimie. 2026;245:120-131. [Content Brief]
- [3]. Giordanetto F, et al. Discovery of AZD2716: A Novel Secreted Phospholipase A2 (sPLA2) Inhibitor for the Treatment of Coronary Artery Disease. ACS Med Chem Lett. 2016;7(10):884-889. Published 2016 Aug 9. [Content Brief]
- [4]. Batsika CS, et al. The design and discovery of phospholipase A2 inhibitors for the treatment of inflammatory diseases. Expert Opin Drug Discov. 2021;16(11):1287-1305. [Content Brief]
- [5]. Hearth JL, et al. In vitro-in vivo discord: A preclinical study of AZD2716 and its racemate with comparison to varespladib for the development of snake venom sPLA2 inhibitors. Toxicon: X. 2026 Feb 12:100243. [Content Brief]
Keywords
