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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Other Sizes |
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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 |
[1]. Bradley JD, et al. A randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol. 2005 Mar;32(3):417-23.
[2]. Lewin M, et al. Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation. Toxins (Basel). 2016 Aug 25;8(9). pii: E248. |
Molecular Formula |
C22H22N2O5
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Molecular Weight |
394.427
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Exact Mass |
394.1529
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CAS # |
172733-08-3
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Related CAS # |
Varespladib;172732-68-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(OC)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3
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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.