| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Varespladib Methyl (LY-333013; A-002; S-3013) is a novel and potent sPLA2 (secretory phospholipase A2) inhibitor with the potential for treating acute coronary syndrome (ACS). It is an orally bioavailable prodrug of varespladib, which inhibits the IIA, V and X isoforms of sPLA2 to reduce inflammation, lower and modulate lipid levels, and reduce levels of C-reactive protein (CRP) and interleukin-6 (IL-6), both indicators of inflammation.
| ln Vitro |
Varespladibmethyl, also known as LY333013, is a prodrug of methanol [1]. When used against 28 medically poisonous snake venom species from six continents, varespladib and its sidewall bioavailable prodrug methylvarespladib (methyl-Varespladib) exhibit high levels of fatal PLA2 (sPLA2) at nanomolar and picomolar concentrations. inhibiting impact [2].
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| References |
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| Additional Infomation |
Varespladib methyl is a methyl ester resulting from the formal condensation of the carboxy group of varespladib with methanol. It is a potential therapy for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s. It has a role as a prodrug, an anti-inflammatory drug, an antidote and an EC 3.1.1.4 (phospholipase A2) inhibitor. It is a methyl ester, an aromatic ether, a member of benzenes, a member of indoles and a primary carboxamide. It is functionally related to a varespladib.
Varespladib methyl has been investigated for the treatment of Acute Coronary Syndrome. Studies showed that Varespladib methyl treatment resulted in significant positive changes on lipoproteins and inflammation. Drug Indication Investigated for use/treatment in atherosclerosis and coronary artery disease. Mechanism of Action A–002 is an orally administered‚ potent inhibitor of secretory phospholipase spla2(spla2)‚ including groups IIA‚ V‚ and X. Atherosclerosis is a disease of the arteries that results from inflammation and the build-up of plaque under the lining of the blood vessel. This build-up can cause vascular swelling and eventual rupture. spla2 levels have been shown to be elevated in patients with both stable and unstable coronary artery disease. Higher levels of the enzyme have been shown to predict an increased risk for future cardiovascular events such as heart attacks and stroke. |
| Molecular Formula |
C22H22N2O5
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|---|---|
| Molecular Weight |
394.427
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| Exact Mass |
394.153
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| CAS # |
172733-08-3
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| Related CAS # |
Varespladib;172732-68-2
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| PubChem CID |
9886917
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| Appearance |
White to off-white solid powder
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| LogP |
3.172
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
604
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VJYDOJXJUCJUHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22N2O5/c1-3-15-20(21(26)22(23)27)19-16(24(15)12-14-8-5-4-6-9-14)10-7-11-17(19)29-13-18(25)28-2/h4-11H,3,12-13H2,1-2H3,(H2,23,27)
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| Chemical Name |
methyl 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate
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| Synonyms |
A002LY-333013 S-3013A002 A-002 LY333013 S3013
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL (~253.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5353 mL | 12.6765 mL | 25.3530 mL | |
| 5 mM | 0.5071 mL | 2.5353 mL | 5.0706 mL | |
| 10 mM | 0.2535 mL | 1.2677 mL | 2.5353 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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