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Submit ReviewASB 14780
Description: Potent and selective cytosolic phospholipase A2 alpha (cPLA2α) inhibitor; active in vivo; orally bioavailable
Chemical Name: 3-(3-Phenethyl-1-(4-phenoxyphenyl)-1H-indol-5-yl)propanoic acid tris salt
Purity: ≥98% (HPLC)
Biological Activity for ASB 14780
ASB 14780 is a potent and selective cytosolic phospholipase A2 alpha (cPLA2α) inhibitor (IC50 = 20 nM). Selective for cPLA2α over secreted PLA2α (sPLA2α; exhibits no inhibition at 10 μM). Inhibits cPLA2α-dependent inflammatory responses in vitro in guinea pig and human whole-blood assays. Improves diet-induced liver injury and CCl4-induced hepatic fibrosis in vivo. Orally bioavailable.
Technical Data for ASB 14780
| M. Wt | 582.7 |
| Formula | C31H27NO3.C4H11NO3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1069046-00-9 |
| PubChem ID | 68519061 |
| InChI Key | MBPXGBINIINSEU-UHFFFAOYSA-N |
| Smiles | NC(CO)(CO)CO.OC(CCC1=CC=C2N(C3=CC=C(C=C3)OC4=CC=CC=C4)C=C(C2=C1)CCC5=CC=CC=C5)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ASB 14780
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 58.27 | 100 |
Preparing Stock Solutions for ASB 14780
The following data is based on the product molecular weight 582.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.72 mL | 8.58 mL | 17.16 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.43 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.72 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets for ASB 14780
References for ASB 14780
References are publications that support the biological activity of the product.
Kanai et al (2016) ASB14780, an orally active inhibitor of group IVA phospholipase A2, is a pharmacotherapeutic candidate for nonalcoholic fatty liver disease. J.Pharmacol.Exp.Ther. 356 604 PMID: 26699145
Tomoo et al (2014) Design, synthesis, and biological evaluation of 3-(1-aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α. J.Med.Chem. 57 7244 PMID: 25102418
If you know of a relevant reference for ASB 14780, please let us know.
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Keywords: ASB 14780, ASB 14780 supplier, ASB14780, AS_B, 14780, potent, selective, cytosolic, group, IVA, phospholipase, A2, alpha, cPLA2a, cPLA2, alfa, inhibitors, inhibits, liver, disease, orally, active, in, vivo, Phospholipases, 6316, Tocris Bioscience
Citations for ASB 14780
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