AS 1842856

Pricing Availability   Qty
Cat.No. 4265 - AS 1842856 | C18H22FN3O3 | CAS No. 836620-48-5
Description: Potent and selective Foxo1 inhibitor; orally bioavailable
Chemical Name: 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

Potent and selective Foxo1 inhibitor (IC50 values are 33 nM at Foxo1 and >1 μM at Foxo3a and Foxo4); decreases Foxo-mediated promoter activity by 70%, 20% and 3% at Foxo1, Foxo4 and Foxo3, respectively. Regulates gluconeogenesis both in vitro and in vivo. Attenuates fasting plasma glucose level in diabetic db/db mice. Also suppresses autophagy, adipocyte differentiation and soluble guanylyl cyclase expression. Orally bioavailable.

Technical Data

M. Wt 347.39
Formula C18H22FN3O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 836620-48-5
PubChem ID 72193864
InChI Key MOMCHYGXXYBDCD-UHFFFAOYSA-N
Smiles CCN1C=C(C(C2=C(C(F)=C(C=C12)NC3CCCCC3)N)=O)C(O)=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 1.74 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 347.39. 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
0.05 mM 57.57 mL 287.86 mL 575.72 mL
0.25 mM 11.51 mL 57.57 mL 115.14 mL
0.5 mM 5.76 mL 28.79 mL 57.57 mL
2.5 mM 1.15 mL 5.76 mL 11.51 mL

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References

References are publications that support the biological activity of the product.

Nagashima et al (2010) Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol.Pharmacol. 78 961 PMID: 20736318

Liu et al (2016) FoxO1 antagonist suppresses autophagy and lipid droplet growth in adipocytes. Cell Cycle 15 2033 PMID: 27260854

Galley et al (2019) Antagonism of forkhead box subclass O transcription factors elicits loss of soluble guanylyl cyclase expression. Mol.Pharmacol. 95 629 PMID: 30988014


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Citations for AS 1842856

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