2839908-40-4

Name	MZ-101/GYS1-IN-2
CAS	2839908-40-4
Molecular Formula	C25H28FN5O2
Molecular Weight	449.52
MOL File	2839908-40-4.mol

Synonyms

MZ-101/GYS1-IN-2 2-Pyrrolidinecarboxamide, 4-fluoro-N-[(S)-[4-(1-methylethyl)phenyl]phenylmethyl]-1-[2-(1H-1,2,3-triazol-5-yl)acetyl]-, (2S,4R)-

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Chemical Properties

Boiling point	738.824±60.00 °C(Press: 760.00 Torr)(predicted)
density	1.285±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
form	Solid
pka	8.987±0.10(predicted)
color	Off-white to light yellow

Hazard Information

Uses

MZ-101 (GYS1-IN-2) is an orally active, potent and selective small-molecule glycogen synthase 1 (GYS1) inhibitor with with an IC50 value of 0.041 μM. MZ-101 reduces glycogen concentrations in cells and in mice. MZ-101 can used to study GYS1 -mediated Pompe disease and other glycogen storage diseases[1][2][3].

in vivo

MZ-101 (2-200 mg/kg, p.o., a single dose for 5 h) inhibits GYS1 but not GYS2 de novo glycogen synthesis and reduces glycogen combined with substrate reduction therapy in WT and Pompe mice^[2].

Animal Model:	Male C57Bl6 mice between 7 and 10 weeks old and male Pompe mice between 10 and 32 weeks old^[2]
Dosage:	2-200 mg/kg
Administration:	p.o., a single dose for 5 h
Result:	Reduced incorporation of glucose into glycogen in skeletal and cardiac muscles of both WT and GAA KO mice in a dose-dependent manner.

References

[1] David John Morgans, et al. Inhibitors of glycogen synthase 1 (gys1) and methods of use thereof. WO2022198196. 2022-09-22.
[2] Ullman JC, et al. Small-molecule inhibition of glycogen synthase 1 for the treatment of Pompe disease and other glycogen storage disorders. Sci Transl Med. 2024 Jan 17;16(730):eadf1691. DOI:10.1126/scitranslmed.adf1691
[3] Gaspar RC, et al. Small molecule inhibition of glycogen synthase I reduces muscle glycogen content and improves biomarkers in a mouse model of Pompe disease. Am J Physiol Endocrinol Metab. 2024 Oct 1;327(4):E524-E532. DOI:10.1152/ajpendo.00175.2024

Supplier

Chunchuang (Wuhan) Technology Co., Ltd

Telephone 15727060112

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList1427518/0_EN.htm

Nantong QuanYi Biotechnology Co., Ltd

Telephone0513-66337626 18051384581

Websitehttps://www.chemhifuture.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Zhengzhou Haode Pharmaceutical Technology Co.,Ltd

Telephone 18037386321

Website

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