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SRI-37330

Chemical Structure : SRI-37330

CAS No.: 2322245-49-6

SRI-37330 (SRI 37330)

Catalog No.: PC-72383Not For Human Use, Lab Use Only.

SRI-37330 (SRI 37330) is an orally available small molecule that regulates TXNIP expression, inhibits endogenous TXNIP mRNA expression (IC50=0.64 uM, INS-1 cells qRT-PCR assays).

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Biological Activity

SRI-37330 (SRI 37330) is an orally available small molecule that regulates TXNIP expression, inhibits endogenous TXNIP mRNA expression (IC50=0.64 uM, INS-1 cells qRT-PCR assays).
SRI-37330 inhibited the activity of the human TXNIP promoter in INS-1 cells by 70% and no cytotoxicity, significantly inhibited TXNIP expression in rat INS-1 cells, primary mouse islets, and isolated human islets.
SRI-37330 significantly changed TXNIP-associated genes, upregulated CTGF, BCL2L1, IGF1R and MAFA, downregualted NLRP1 and MLXIPL, in INS-1 cells.
SRI-37330 effectively inhibited polymerase II (Pol II) binding to the E-box motif region of the TXNIP promoter, but not to an upstream TXNIP promoter region or to an established Pol II binding site in the insulin receptor substrate 2 (IRS2).
SRI-37330 lowers serum glucagon levels, inhibits hepatic glucose production and improves glucose homeostasis in mice (100 mg/kg/day in the drinking water).

Physicochemical Properties

M.Wt 424.867
Formula C16H20ClF3N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

50 mg/mL (DMSO)

Chemical Name/SMILES

N-((1-(6-(trifluoromethyl)quinazolin-4-yl)piperidin-3-yl)methyl)methanesulfonamide hydrochloride

References

1. Lance A Thielen, et al. Cell Metab. 2020 Sep 1;32(3):353-365.e8.

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