Gitogenin 

Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC₅₀ values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms^[1][2].

IC50: 0.69 µM (UDP-glucuronosyltransferase 1A4)^[1]; IC50: 37.2 μM (α-glucosidase)^[2]

When tamoxifen is used as the substrate metabolized by UGT1A4 in HLMs, Gitogenin exhibits potent inhibition of tamoxifen, with an IC₅₀ value of 6.13 µM. Similarly, for midazolam as the substrate of UGT1A4, the IC₅₀ value is 5.7 µM. In addition, when olanzapine is used as a substrate of UGT1A4, the IC₅₀ value is determined as 6.0 µM. Finally, we also evaluats Gitogenin for asenapine glucuronidation mediated by UGT1A4, and similar inhibition effect is observed, with an IC₅₀ value of 22.0 µM^[1].

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

Stimulation of growth hormone release is investigated on rat pituitary cells in vitro. Gitogenin (20 μg/mL) shows rat growth-hormone (rGH) release stimulating activities (26.1 ng/mL)^[3].

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

432.64

C₂₇H₄₄O₄

511-96-6

Solid

White to off-white

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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]. Xu M, et al. Drug interaction study of natural steroids from herbs specifically toward human UDP-glucuronosyltransferase (UGT) 1A4 and their quantitative structure activity relationship (QSAR) analysis for prediction. Pharmacol Res. 2016 Aug;110:139-150.  [Content Brief]

  [2]. Xu M, et al. Drug interaction study of natural steroids from herbs specifically toward human UDP-glucuronosyltransferase (UGT) 1A4 and their quantitative structure activity relationship (QSAR) analysis for prediction. Pharmacol Res. 2016 Aug;110:139-150.

  [3]. Naveed MA, et al. Longipetalosides A-C, new steroidal saponins from Tribulus longipetalus. Steroids. 2014 May;83:45-51.  [Content Brief]

  [4]. Shim SH, et al. Rat growth-hormone release stimulators from fenugreek seeds. Chem Biodivers. 2008 Sep;5(9):1753-61.  [Content Brief]