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| ln Vitro |
The RA-induced rise in MUC16 protein seen in cell lysates at both time intervals was entirely suppressed by vespladib sodium (10 μM; 24 and 48 hours; HCjE cells) therapy [2]. With an inhibition rate of 100% at 24 hours and 99% at 48 hours, vespladib sodium (10 μM) administration can strongly suppress RA-induced MUC16 expression in HCjE cells [2].
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| ln Vivo |
An IC50 of 0.79 μM is observed for the inhibition of human sPLA2-induced thromboxane A2 (TXA2) release from guinea pig lung bronchial lavage cells upon varespladibodium administration. Varespladib sodium has an ED50 of 16.1 mg/kg[1].
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| Cell Assay |
Western Blot analysis [2]
Cell Types: HCjE Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: RA-induced MUC16 protein expression was Dramatically inhibited at both time points. RT-PCR[2] Cell Types: HCjE Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Dramatically inhibited RA-induced MUC16 expression, reaching 100% at 24 hrs (hours) and 99% at 48 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: Male Hartley guinea pig (300-500 g) [1]
Doses: 3 mg/kg, 10 mg/kg and 30 mg/kg Route of Administration: intravenous (iv) (iv)injection (pharmacokinetic/PK/PK study) Experimental Results: sPLA2 activity in BAL Sustained inhibition of liquid was observed. diminished human sPLA2-induced TXA2 production on guinea pig BAL cells. |
| 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. 1
[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 |
C21H19N2NAO5
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|---|---|
| Molecular Weight |
402.375736474991
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| CAS # |
172733-42-5
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| Related CAS # |
Varespladib;172732-68-2
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| SMILES |
[Na+].O(CC(=O)[O-])C1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC1C=CC=CC=1
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4852 mL | 12.4261 mL | 24.8521 mL | |
| 5 mM | 0.4970 mL | 2.4852 mL | 4.9704 mL | |
| 10 mM | 0.2485 mL | 1.2426 mL | 2.4852 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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