Varespladib
Varespladib
CAS: 172732-68-2
Molecular Formula: C21H20N2O5
Varespladib - Names and Identifiers
| Name | Varespladib |
| Synonyms | LY315920 LY-333013 Varepladib Varespladib VARESPLADIB UNII-2Q3P98DATH LY315920(Varespladib) Varespladib (LY315920) ((3-(Aminooxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yl)oxy)acetic acid ({3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl}oxy)acetic acid sodium ({3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl}oxy)acetate 2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yloxy)acetic acid [[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid Acetic acid, ((3-(aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl)oxy)-, 2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]Acetic Acid |
| CAS | 172732-68-2 |
| EINECS | 1592732-453-0 |
| InChI | InChI=1/C21H20N2O5.Na/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);/q;+1/p-1 |
Varespladib - Physico-chemical Properties
| Molecular Formula | C21H20N2O5 |
| Molar Mass | 380.39 |
| Density | 1.32±0.1 g/cm3(Predicted) |
| Melting Point | 230-234 °C |
| Boling Point | 667.9±65.0 °C(Predicted) |
| Flash Point | 357.7°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Vapor Presure | 9.53E-19mmHg at 25°C |
| Appearance | powder |
| Color | white to beige |
| pKa | 3.12±0.40(Predicted) |
| Storage Condition | -20°C |
| In vitro study | LY315920 significantly inhibited sPLA2 activity in serum of many different species, including Rat, rabbit, guinea pig and human, with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. LY315920 acts on BAL cells lacking human sPLA2 in a dose range of 0.1 μm to 3 μm to reduce human sPLA2-regulated thrombosis in a concentration-dependent manner with an IC50 of about 0.8 μm. LY315920 (10 μm) significantly inhibited the expression of membrane-associated mucin MUC16 induced by all-trans-retinoic acid (RA) in Human conjunctival epithelial cell line (HCjE) by 100% at 24 hours, 99% inhibition at 48 hours. |
| In vivo study | In vitro, LY315920 inhibits human sPLA2-induced thrombus release from Guinea pig BAL cells at doses of 3 mg/kg to 30 mg/kg I. V. The ED50 was 16.1 mg/kg. LY315920 was administered orally or intravenously at a dose of 0.3 mg/kg-3 mg/kg to abrogate serum sPLA2 activity in transgenic mice expressing human sPLA2 in a dose-and time-dependent manner. |
Varespladib - Risk and Safety
| WGK Germany | 3 |
Varespladib - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.629 ml | 13.144 ml | 26.289 ml |
| 5 mM | 0.526 ml | 2.629 ml | 5.258 ml |
| 10 mM | 0.263 ml | 1.314 ml | 2.629 ml |
| 5 mM | 0.053 ml | 0.263 ml | 0.526 ml |
Last Update：2024-01-02 23:10:35
Varespladib - Reference Information
| biological activity | Varespladib (LY315920) is an effective, selective human non-pancreatic secretory phospholipase A2 (hnsPLA)(human non-pancreatic secretory phospholipase A2) inhibitor, IC50 is 7 nM. Phase 3. |
| target | TargetValue hnsPLA2 (Cell-free say) 7 nM |
| Target | Value |
| hnsPLA2 (Cell-free assay) | 7 nM |
| in vitro study | LY315920 acts on the serum of many different species, including rats, rabbits, guinea pigs and humans, significantly inhibiting sPLA2 activity, IC50 is 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM respectively. LY315920 acts on BAL cells lacking human sPLA2 in the dose range of 0.1 μM-3 μM to reduce thrombosis regulated by human sPLA2. This effect is concentration dependent, with IC50 of about 0.8 μM. LY315920 (10 μM) acts on human conjunctival epithelial cell line (HCjE) to significantly inhibit all-trans-retinoic acid (RA)-induced expression of membrane-associated mucin MUC16, inhibit 100% at 24 hours and inhibit 99% at 48 hours. |
| in vivo study | in vitro, LY315920 treated by intravenous injection at a dose of 3 mg/kg to 30 mg/kg, inhibit the thrombus released from guinea pig BAL cells induced by human sPLA2. ED50 is 16.1 mg/kg. LY315920 treated transgenic mice expressing human sPLA2 at doses of 0.3 mg/kg-3 mg/kg orally or intravenously, serum sPLA2 activity was abolished. This effect was dose-and time-dependent. |
Last Update：2024-04-09 02:00:00
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