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Purity: ≥98%
Varespladib (formerly A-002; A 002; LY315920; LY-315920) is a investigational drug with the potential for treating inflammatory diseases such as acute coronary syndrome and acute chest syndrome as well as snakebite. It works as s selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM.
| ln Vitro |
The RA-induced rise in MUC16 protein seen in cell lysates at both time intervals was entirely suppressed by vindespladib (10 μM; 24 and 48 hours; HCjE cells) therapy [2]. Treatment with varaspladib (10 μM; 24 and 48 hours; HCjE cells) dramatically reduced the amount of MUC16 that was produced by RA by 100% at 24 hours and 99% at 48 hours [2].
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| ln Vivo |
At an IC50 of 0.79 μM, varespladib therapy prevents human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells. 16.1 mg/kg is the ED50 for vespladib[1].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: HCjE cells Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: Dramatically inhibited the RA-induced MUC16 protein expression at both time points. RT-PCR[2] Cell Types: HCjE cells Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) and 48 hrs (hours) Experimental Results: Dramatically inhibited RA-induced MUC16 expression by 100% at 24 hrs (hours) and 99% at 48 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: Male Hartley guinea pigs (300-500 g)[1]
Doses: 3 mg/kg, 10 mg/kg, and 30 mg/kg Route of Administration: intravenous (iv) injection (pharmacokinetic/PK study) Experimental Results: Consistent inhibition of sPLA2 activity in BAL fluid was observed. decreased the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs. |
| References |
[1]. Snyder DW, et al. 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 Mar;288(3):1117-24.
[2]. Hori Y, et al. Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61. |
| Molecular Formula |
C21H20N2O5
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|---|---|
| Molecular Weight |
380.39
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| CAS # |
172732-68-2
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| Related CAS # |
Varespladib sodium;172733-42-5;Varespladib methyl;172733-08-3
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| SMILES |
NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O
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| InChi Key |
BHLXTPHDSZUFHR-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-((3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yl)oxy)acetic acid
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| Synonyms |
A002; A 002; LY315920; Varespladib; LY-315920; LY 315920; A-002;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6289 mL | 13.1444 mL | 26.2888 mL | |
| 5 mM | 0.5258 mL | 2.6289 mL | 5.2578 mL | |
| 10 mM | 0.2629 mL | 1.3144 mL | 2.6289 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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