Isosinensetin 

Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC₅₀: 2.61 µM; K_i: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc^{[1][2][3][4][5]}.

Isosinensetin (0.1-100 μM; 4-24 h) can significantly inhibit P-gp (IC₅₀: 4.2 μM), and increase the cytotoxicity induced by paraquat in MDR1-MDCKII cells^[1].
Isosinensetin (250 μg/mL) can inhibit erythrocyte hemolysis with an inhibition rate of 92.08%^[2].
Isosinensetin (40-80 μM; 1 h) can increase the intracellular calcium ion concentration, promote the expression of hTAS2R50 and proglucagon, and stimulate the secretion of GLP-1 in NCI-H716 cells ^[3].
Isosinensetin (0-10 μM; 0-7 days) can inhibit the formation of osteoclasts and their bone resorption function in BMMs. The mechanism involves the inhibition of the ROS-mediated NF-κB/MAPK signaling pathway^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Isosinensetin (5-10 mg/kg; intraperitoneal injection; once every two days; 6 weeks) alleviates estrogen deficiency-induced osteoporosis in mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

372.37

C₂₀H₂₀O₇

17290-70-9

Solid

Off-white to light yellow

O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=C(OC)C(OC)=CC(OC)=C13

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bai J, et al. Inhibitory effects of flavonoids on P-glycoprotein in vitro and in vivo: Food/herb-drug interactions and structure-activity relationships. Toxicol Appl Pharmacol. 2019 Apr 15;369:49-59.  [Content Brief]

  [2]. Jiang Y, et al. Isolation of adenosine, iso-sinensetin and dimethylguanosine with antioxidant and HIV-1 protease inhibiting activities from fruiting bodies of Cordyceps militaris. Phytomedicine. 2011 Jan 15;18(2-3):189-93.  [Content Brief]

  [3]. Lee SH, et al. Isosinensetin Stimulates Glucagon-like Peptide-1 Secretion via Activation of hTAS2R50 and the Gβγ-Mediated Signaling Pathway. Int J Mol Sci. 2023 Feb 12;24(4):3682.  [Content Brief]

  [4]. Qin Y, et al. Isosinensetin alleviates estrogen deficiency-induced osteoporosis via suppressing ROS-mediated NF-κB/MAPK signaling pathways. Biomed Pharmacother. 2023 Apr;160:114347.  [Content Brief]

  [5]. Trang N M, et al. Inhibition of PTP1B by isosinensetin, a polymethoxylated flavone isolated from trifoliate orange peel: Kinetic studies, molecular docking, and molecular dynamics simulation. Chemical Papers, 2023, 77(3): 1751-1757.