JY-2

• CAT Number: I041290
• CAS Number: 339103-05-8
• Molecular Formula: C13H7Cl2N3O
• Molecular Weight: 292.12
• Purity: ≥95%
• Synonyms: 5-(2,4-dichlorophenyl)-3-pyridin-2-yl-1,2,4-oxadiazole
• InChI: InChI=1S/C13H7Cl2N3O/c14-8-4-5-9(10(15)7-8)13-17-12(18-19-13)11-3-1-2-6-16-11/h1-7H
• InChIKey: WBMHQMQALJDGHI-UHFFFAOYSA-N
• SMILES: C1=CC=NC(=C1)C2=NOC(=N2)C3=C(C=C(C=C3)Cl)Cl

JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity[1].
JY-2 (10-100 μM; 24 h) reduces palmitic acid (PA; HY-N0830)-induced lipotoxicity in HepG2 and INS-1 cells[1].
JY-2 (50-200 mg/kg; oral; 3 times for two days or daily for 4 weeks) shows anti-diabetic effects in mice[1].
Pharmacokinetic parameters of JY-2[1]

Parameters
i.v. (20 mg/kg)
p.o. (50 mg/kg)

AUCall (ng·h/mL)
5017 ± 1038
12270 ± 2775

AUCinf.obs (ng·h/mL)
5030 ± 1037
12400 ± 2753

Cmax (ng/mL)
10790 ± 3269
6826 ± 2342

Tmax (h)
0.1 ± 0.1
0.8 ± 0.7

T1/2 (h)
0.8 ± 0.2
1.3 ± 0.4

MRTinf.obs (h)
0.7 ± 0.1
2.0 ± 0.1

F (%)

97.8

Reference

[1]. Choi HE, et al. Novel FoxO1 inhibitor, JY-2, ameliorates palmitic acid-induced lipotoxicity and gluconeogenesis in a murine model. Eur J Pharmacol. 2021 May 15;899:174011.
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