172733-42-5
172733-42-5 structure
- Name: Varespladib sodium
- Chemical Name: sodium,2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate
- CAS Number: 172733-42-5
- Molecular Formula: C21H19N2NaO5
- Molecular Weight: 402.37600
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
- Create Date: 2017-01-16 23:26:59
- Modify Date: 2024-01-09 06:02:57
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Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1].
| Name | sodium,2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate |
|---|---|
| Synonyms |
UNII-F6M52CDT0W
Varespladib sodium |
| Description | Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
sPLA2:9 nM (IC50) |
| In Vitro | Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points[2]. Varespladib sodium (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours[2]. Western Blot Analysis[2] Cell Line: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited the RA-induced MUC16 protein expression at both time points. RT-PCR[2] Cell Line: HCjE cells Concentration: 10 μM Incubation Time: 24 hours, 48 hours Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours. |
| In Vivo | Varespladib sodium treatment inhibits human sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. And the ED50 for Varespladib sodium is 16.1 mg/kg[1]. Animal Model: Male Hartley guinea pigs (300-500 g)[1] Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg Administration: Intravenous injection (Pharmacokinetic study) Result: Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs. |
| References |
| Molecular Formula | C21H19N2NaO5 |
|---|---|
| Molecular Weight | 402.37600 |
| Exact Mass | 402.11900 |
| PSA | 114.45000 |
| LogP | 1.74900 |
|
~%
172733-42-5 |
| Literature: SHIONOGI and CO., LTD.; ELI LILLY AND COMPANY Patent: EP1058547 B1, 2005 ; Location in patent: Page/Page column 5 ; |
