LY311727
- Product Name
- LY311727
- CAS No.
- 164083-84-5
- Chemical Name
- LY311727
- Synonyms
- LY 311727;3-(1-Benzyl-2-ethyl-3-carboxamido-methyl-indol-5-yl)-oxy-propan-ephosphonic acid;(3-{[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid;[3-[[3-(2-Amino-2-oxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-5-yl]oxy]propyl]-phosphonicacid;(3-{[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid (ApexBio);Phosphonic acid, P-[3-[[3-(2-aMino-2-oxoethyl)-2-ethyl-1-(phenylMethyl)-1H-indol-5-yl]oxy]propyl]-
- CBNumber
- CB02518822
- Molecular Formula
- C22H27N2O5P
- Formula Weight
- 430.43
- MOL File
- 164083-84-5.mol
LY311727 Property
- Boiling point:
- 758.2±70.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥15mg/mL
- pka
- 2.43±0.10(Predicted)
- form
- powder
- color
- white to tan
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- 17973
- Product name
- LY311727
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 17973
- Product name
- LY311727
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $127
- Updated
- 2024/03/01
- Product number
- 17973
- Product name
- LY311727
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $231
- Updated
- 2024/03/01
- Product number
- L486640
- Product name
- LY311727
- Packaging
- 25mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- 255724
- Product name
- LY 311727
- Packaging
- 10mg
- Price
- $480
- Updated
- 2021/12/16
LY311727 Chemical Properties,Usage,Production
Description
Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids. Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling. LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 μM) that interacts with the active site of the enzyme in a non-covalent manner. It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2). LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.
Uses
LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 μM) that interacts with the active site of the enzyme in a non-covalent manner. It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2). LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.[Cayman Chemical]
Uses
LY 311727 is an inhibitor of secretory phospholipase A2 (sPLA2) and can be used to block Pseudomonas aeruginosa cytotoxicity. It can also attenuate VEGF-mediated platelet-activating factor (PAF) synthesis in HUVEC and BAEC cells.
Biochem/physiol Actions
LY311727 is an orally active; potent secretory Phospholipase A2 (sPLA2; Group IIa) inhibitor.
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[2].
| Animal Model: | C57BL/6J mice, Mt-sPLA2 transgenic mice model[2] |
| Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Intravenous injection |
| Result: | Significantly and dose dependently suppressed the PLA2 activity in the serum. |
References
[1] C. DONG. Total direct chemical synthesis and biological activities of human group IIA secretory phospholipase A2.[J]. The Ukrainian Biochemical Journal, 2002, 110 1: 505-511. DOI: 10.1042/bj20011648
[2] R.W. SCHEVITZ. Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2[J]. Nature Structural & Molecular Biology, 1995, 2 6: 458-465. DOI: 10.1038/nsb0695-458
[3] E HURT-CAMEJO. Localization of nonpancreatic secretory phospholipase A2 in normal and atherosclerotic arteries. Activity of the isolated enzyme on low-density lipoproteins.[J]. Arteriosclerosis, Thrombosis, and Vascular Biology, 1997, 17 2: 300-309. DOI: 10.1161/01.atv.17.2.300
[4] L THOMMESEN. Selective inhibitors of cytosolic or secretory phospholipase A2 block TNF-induced activation of transcription factor nuclear factor-kappa B and expression of ICAM-1.[J]. Journal of immunology, 1998, 161 7: 3421-3430.
[5] H SHINOHARA. Regulation of delayed prostaglandin production in activated P388D1 macrophages by group IV cytosolic and group V secretory phospholipase A2s.[J]. The Journal of Biological Chemistry, 1999, 274 18: 12263-12268. DOI: 10.1074/jbc.274.18.12263
[6] J BALSINDE. Group V phospholipase A(2)-dependent induction of cyclooxygenase-2 in macrophages.[J]. The Journal of Biological Chemistry, 1999, 274 37: 25967-25970. DOI: 10.1074/jbc.274.37.25967
LY311727 Preparation Products And Raw materials
Raw materials
Preparation Products
LY311727 Suppliers
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15838
- Advantage
- 69
- Tel
- 021-61415566 800-8193336
- orderCN@merckgroup.com
- Country
- China
- ProdList
- 51395
- Advantage
- 80
- Tel
- 888-539-0666
- Fax
- 888-539-0666
- info@emmx.com
- Country
- United States
- ProdList
- 8447
- Advantage
- 60
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 021-69568360 18916172912
- order@med-bio.cn
- Country
- China
- ProdList
- 8140
- Advantage
- 58
- Tel
- 021-58432009 400-005-6266
- Fax
- 021-58436166
- marketing@energy-chemical.com
- Country
- China
- ProdList
- 44918
- Advantage
- 58
- Tel
- 028-83243028 19136088901
- sinostandards@163.com
- Country
- China
- ProdList
- 4976
- Advantage
- 58
- Tel
- 010-60605840 15801484223;
- psaitong@jm-bio.com
- Country
- China
- ProdList
- 29757
- Advantage
- 58
- Tel
- 15921930842 15921930842
- yh-wang@univ-bio.com
- Country
- China
- ProdList
- 25004
- Advantage
- 58