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伐瑞拉迪

规格或纯度: ≥98%

CAS编号: 172732-68-2
分子式: C₂₁H₂₀N₂O₅
分子量: 380.39
PubChem编号: 155815

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货号 (SKU)	包装规格	是否现货
V125011-5mg	5mg	现货
V125011-10mg	10mg	现货
V125011-50mg	50mg	现货

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sPLA2-2A Inhibitor

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基本描述

规格或纯度	≥98%
英文名称	Varespladib
别名	伐瑞拉迪
英文别名	[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid;LY 315920;LY315920;LY-315920
生化机理	Varespladib (LY 315920), a specifically designed indolic secretory phospholipase A2 (sPLA2) inhibitor, has shown promising results in animals and adults. Inhibition seems to be inversely related to the severity of gas exchange impairment. Varespladib acts synergistically with pravastatin to decrease atherosclerosis, possibly throμgh decreased levels of systemic inflammation or decreased lipid levels. Varespladib treatment also resulted in a profound increase in plasma PON activity and significantly larger fibrous caps, sμggesting the formation of more stable plaque architecture.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	5mg、10mg卖完停产，不再备货
产品介绍	Varespladib (LY315920)是一种有效的，选择性的human non-pancreatic secretory phospholipase A2 (hnsPLA)（人类非胰腺分泌型磷脂酶A2）抑制剂，IC50为7 nM。 Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM.

名称和标识符

IUPAC Name	2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid
INCHI	InChI=1S/C21H20N2O5/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25)
InChi Key	BHLXTPHDSZUFHR-UHFFFAOYSA-N
Canonical SMILES	CCC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OCC(=O)O)C(=O)C(=O)N
分子式	C₂₁H₂₀N₂O₅
PubChem CID	155815
分子量	380.39

数据库链接

PubChem CID	155815
CAS Registry No.	172732-68-2
ChEMBL Ligand	CHEMBL148674
BindingDB Ligand	50055366
RCSB PDB Ligand	VRD

化学和物理性质

溶解性	DMSO 76 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

安全信息

WGK Germany	3

靶标

Target ID

1417

名称

sPLA₂-2A

缩写名

SHP2

家族

Phospholipase A₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	144	1p36.13	PLA2G2A	phospholipase A2 group IIA
Mouse	2	146	4 70.57 cM	Pla2g2a	phospholipase A2, group IIA (platelets, synovial fluid)
Rat	2	146	5q36	Pla2g2a	phospholipase A2 group IIA

Ensembl Gene

ENSG00000188257 (Hs) , ENSMUSG00000058908 (Mm) , ENSRNOG00000016945 (Rn)

Entrez Gene

18780 (Mm) , 29692 (Rn) , 5320 (Hs)

OMIM

172411 (Hs)

Protein GI

239915991 (Hs) , 132626633 (Mm) , 291621686 (Rn)

UniProtKB

P14555 (Hs) , P14423 (Rn) , P31482 (Mm)

RefSeq Nucleotide

NM_000300 (Hs) , NM_001082531 (Mm) , NM_031598 (Rn)

RefSeq Protein

NP_000291 (Hs) , NP_001076000 (Mm) , NP_113786 (Mm)

DrugBank Target

P14555 (Hs)

CATH/Gene3D

1.20.90.10 (N/A)

ChEMBL Target

CHEMBL5761 (Mm) , CHEMBL3686 (Rn) , CHEMBL3474 (Hs)

关联配体

Ligand ID	9657
名称	varespladib
别名	LY315920
类别	Synthetic organic
学名	2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid
生物活性评价	Varespladib does not inhibit human cytosolic phospholipase A₂, thromboxane synthase or cyclooxygenase enzymes .
评价	Varespladib (LY315920) is a secretory phospholipase A2 (sPLA₂) inhibitor in clinical development. The administered form can be varespladib sodium (A-001, for intravenuous administration) or varespladib methyl (A-002, for oral administration). The history of varespladib's discovery and development is summarized in .
临床描述	The objective of this study is to evaluate the safety and efficacy of short-term A-002 treatment on morbidity and mortality when added to atorvastatin and standard of care in subjects with an acute coronary syndrome (ACS). The purpose of this study is to determine the effectiveness of A 001 infusion in preventing acute chest syndrome in sickle cell disease (SCD) subjects with vaso-occlusive crisis, fever, and elevated serum C-reactive protein (CRP).
来源公司	Anthera Pharmaceuticals Anthera Pharmaceuticals

参考文献

1. Snyder DW, Bach NJ, Dillard RD, Draheim SE, Carlson DG, Fox N, Roehm NW, Armstrong CT, Chang CH, Hartley LW et al.. (1999) Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI.. J Pharmacol Exp Ther, 288 (3): (1117-24). [PMID:10027849]
2. Sanford M, McCormack PL. (2011) Varespladib.. Am J Cardiovasc Drugs, 11 (2): (137-43). [PMID:21446779]
3. Draheim SE, Bach NJ, Dillard RD, Berry DR, Carlson DG, Chirgadze NY, Clawson DK, Hartley LW, Johnson LM, Jones ND et al.. (1996) Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.. J Med Chem, 39 (26): (5159-75). [PMID:8978844]