ASB 14780

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Cat.No. 6316 - ASB 14780 | C31H27NO3.C4H11NO3 | CAS No. 1069046-00-9
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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 58.27 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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References

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


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Citations for ASB 14780

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