VARESPLADIB

Product Name: VARESPLADIB
CAS No.: 172732-68-2
Chemical Name: VARESPLADIB
Synonyms: LY315920;CS-68;CS-2393;LY-333013;VARESPLADIB;Varespladib, >98%;LY315920(Varespladib);Varespladib (LY315920);LY315920;LY-315920 ;LY 315920;Varespladib LY315920 LY-315920
CBNumber: CB31011677
Molecular Formula: C21H20N2O5
Formula Weight: 380.39
MOL File: 172732-68-2.mol

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VARESPLADIB Property

Melting point:: 230-234 °C
Boiling point:: 667.9±65.0 °C(Predicted)
Density: 1.32±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: DMSO (Slightly), Methanol (Slightly)
form: powder
pka: 3.12±0.40(Predicted)
color: white to beige

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1100
Product name: Varespladib
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $118
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML1100
Product name: Varespladib
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $476
Updated: 2024/03/01

Cayman Chemical

Product number: 18267
Product name: LY315920
Purity: ≥95%
Packaging: 5mg
Price: $86
Updated: 2024/03/01

Cayman Chemical

Product number: 18267
Product name: LY315920
Purity: ≥95%
Packaging: 10mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 18267
Product name: LY315920
Purity: ≥95%
Packaging: 25mg
Price: $379
Updated: 2024/03/01

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VARESPLADIB Chemical Properties,Usage,Production

Uses

Varespladib has been used as a secretory phospholipase A (sPLA2) inhibitor:

to test its effect on the human astrocytes subjected to psychosine-induced toxicity
to test its neutralization functionality on the black snake species P. colletti?venom
in combination with snake venom metalloproteinases (SVMP)-inhibitor, marimastat to test its protective functionality on envenoming by vipers

Uses

VARESPLADIB is used as a PLA2 inhibitor (Phospholipase A2 Enzyme inhibitor).

Definition

ChEBI: Varespladib is a member of the class of indoles that is 1H-indole substituted by benzyl, ethyl, oxamoyl, and carboxymethoxy groups at positions 1, 2, 3, and 4, respectively. It is an oral secretory phospholipase A2 inhibitor and exhibits anti-inflammatory effects. It has a role as an EC 3.1.1.4 (phospholipase A2) inhibitor, an anti-inflammatory drug and an antidote. It is a member of indoles, a member of benzenes, an aromatic ether, a dicarboxylic acid monoamide, a monocarboxylic acid and a primary carboxamide. It is a conjugate acid of a varespladib(1-).

Biological Activity

phospholipases (plas) produce rate-limiting precursors in the various types of biologically active lipid biosynthesis. increased levels of human nonpancreatic secretory phospholipase a2 (hnps-pla2) have been detected in several pathological conditions. ly315920 was selected for evaluation clinically as an hnps-pla2 inhibitor.

Biochem/physiol Actions

Varespladib is effective against viper and elapid venoms and is used in snakebite therapy. It is reported to interact with the hydrophobic channel of the PLA2-like toxin in in vitro structural studies. It blocks inflammatory cascades related to the sPLA2.

in vitro

the true potency of ly315920 was defined to be a mole fraction of 1.5 x 10-6 using a deoxycholate/phosphatidylcholine assay. ly315920 was found to be 40-fold less active against human, group ib, pancreatic spla2 and was inactive against cytosolic pla2 and the constitutive and inducible forms of cyclooxygenase. human spla2-induced thromboxane a2 release from isolated guinea pig lung bronchoalveolar lavage cells was inhibited by ly315920 with the ic50 of 0.79 μm [1].

in vivo

the i.v. administration of ly315920, 5 min before the bronchoalveolar lavage cells harvest, led to the inhibition of spla2-induced production of txa2 with an ed50 of 16.1 mg/kg. [2].

IC 50

9 ± 1 nm or 7.3 x 10-6 mole fraction for spla2 activity

References

[1] snyder dw, bach nj, dillard rd, draheim se, carlson dg, fox n, roehm nw, armstrong ct, chang ch, hartley lw, johnson lm, roman cr, smith ac, song m, fleisch jh. 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. 1999;288(3):1117-24.
[2] rosenson rs, hislop c, elliott m, stasiv y, goulder m, waters d. effects of varespladib methyl on biomarkers and major cardiovascular events in acute coronary syndrome patients. j am coll cardiol. 2010;56(14):1079-88.

VARESPLADIB Preparation Products And Raw materials

Raw materials

Preparation Products

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VARESPLADIB Suppliers

Canada 1 China 118 United Kingdom 1 United States 21 Global 141

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4863
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AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2784
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ApexBio Technology LLC

Tel: +1-832-696-8203
Fax: +1-832-641-3177
Email: info@apexbt.com
Country: United States
ProdList: 477
Advantage: 60

Target molecule Corp.

Tel: 857-239-0968
Fax: 857-239-8801
Email: service1@targetmol.com
Country: United States
ProdList: 2559
Advantage: 60

Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
Email: info@musechem.com
Country: United States
ProdList: 4662
Advantage: 60

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 19892
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InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6393
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Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
ProdList: 2738
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Aladdin Scientific

Tel: +1-833-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57511
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BOC Sciences

Tel: 16314854226
Email: info@bocsci.com
Country: United States
ProdList: 9926
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View Lastest Price from VARESPLADIB manufacturers

Shaanxi Dideu Medichem Co. Ltd

Product: VARESPLADIB 172732-68-2
Price: US $0.00-0.00/KG
Min. Order: 5mg
Purity: 99%
Supply Ability: 2000tons
Release date: 2019-12-31

Career Henan Chemical Co

Product: VARESPLADIB 172732-68-2
Price: US $5.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 1ton
Release date: 2019-09-03

172732-68-2, VARESPLADIBRelated Search:

4-HYDROXY-1H-INDOLE-3-CARBALDEHYDE 4-Hydroxy-2-methylindole 1-BENZYLPYRROLE-3-CARBOXALDEHYDE 4-METHOXY-1-METHYLINDOLE 4-Hydroxytryptamine 1-(1-ETHYL-1H-INDOL-3-YL)ETHANONE VARESPLADIB ASISCHEM R42031 2-(1-BENZYL-1H-INDOL-3-YL)-ETHYLAMINE 1-BENZYL-1H-INDOLE-3-CARBALDEHYDE 4-methoxy-2-methyl-1H-indole 4-Methoxyindole-3-carboxaldehyde (3-AMINOOXALYL-1-BENZYL-2-ETHYL-1H-INDOL-4-YLOXY)-ACETIC ACID METHYL ESTER CHEMBRDG-BB 5102396

VARESPLADIB

LY315920(Varespladib)

2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]Acetic Acid

[[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid

LY315920

LY-333013

Varespladib (LY315920)

2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yloxy)acetic acid

2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid

CS-2393

Varespladib, >98%

LY315920;LY-315920 ;LY 315920

CS-68

Acetic acid, 2-[[3-(2-amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-

2-{[1-benzyl-3-(carbamoylcarbonyl)-2-ethyl-1H-ind ol-4-yl]oxy}acetic acid

Varespladib LY315920 LY-315920

172732-68-2

C21H19N2NaO5

Inhibitor

Inhibitors