Steviol glucuronide
Steviol glucuronide is a metabolite of Steviol (HY-N2057). Steviol glucuronide upregulates Glucagon receptor transcription and downregulates β-2-microglobulin transcription. Steviol glucuronide scavenges hydroxyl/superoxide radicals and reduces thiobarbituric acid reactive substances, without DPPH/nitric oxide scavenging activity. Steviol glucuronide stimulates glucose-dependent insulin secretion and does not affect basal insulin under low-glucose conditions. Steviol glucuronide enters cells via passive diffusion and OAT3/OATP1B1/OATP1B3/OATP2B1-mediated uptake, and inhibits OATP1B1/OATP1B3-mediated transport of Rosuvastatin (HY-17504B). Steviol glucuronide can be used in research on type 2 diabetes.
For research use only. We do not sell to patients.
- CAS No.: 885044-59-7
- Formula: C26H38O9
- Molecular Weight:494.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
26.4 μM
|
Inhibition of OATP1B1-mediated uptake of 1 μM rosuvastatin in HEK293 cells after 30 min preincubation at 37°C measured by LC-MS/MS.
Inhibition of OATP1B1-mediated uptake of 1 μM rosuvastatin in HEK293 cells after 30 min preincubation at 37°C measured by LC-MS/MS.
|
26525112 |
| HEK293 | IC50 |
39.8 μM
|
Inhibition of OATP1B3-mediated uptake of 1 μM rosuvastatin in HEK293 cells after 30 min preincubation at 37°C measured by LC-MS/MS.
Inhibition of OATP1B3-mediated uptake of 1 μM rosuvastatin in HEK293 cells after 30 min preincubation at 37°C measured by LC-MS/MS.
|
26525112 |
In Vitro
Steviol glucuronide (0.1 μM; 72 h) alters the transcription of B2m and Gcgr in isolated mouse pancreatic islets after 72 h and produces numerical increases in Pdk1, Nkx2-2, Pdx1, Nkx6.1, Akt1, and Insr[1].
Steviol glucuronide scavenges superoxide radicals in the cell-free NBT/NADH/PMS assay, with an IC50 of 0.211 mM[2].
Steviol glucuronide (30 min) shows no DPPH radical scavenging activity in the cell-free DPPH assay[2].
Steviol glucuronide (25°C, protected from light for 150 min) shows no NO free radical scavenging activity in the cell-free sodium nitroprusside/Griess assay[2].
Steviol glucuronide has an uptake Km of 143.3 µM in HEK293-OAT3 cells and exhibits the highest intrinsic clearance (2.64 µl/min/mg protein) among the uptake transporters tested[4].
Steviol glucuronide (0-300 µM; 30 min) inhibits the uptake of Rosuvastatin (HY-17504B) by HEK293-OATP1B1 and -OATP1B3 cells, with IC50 values of 26.4 and 39.8 µM, respectively, and weakly inhibits OAT3-mediated uptake[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse pancreatic islets
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Concentration:0.1 μM
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Incubation Time:72 h
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Result:Significantly decreased transcript level of beta‐2‐microglobulin (B2m) and significantly increased transcript level of glucagon receptor by 102% (Gcgr).
Upregulated transcript level of pyruvate dehydrogenase kinase, isoenzyme 1 (Pdk1), nearly reached a significant level.
Chemical Information
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CAS No. 885044-59-7
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Molecular Weight 494.57
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Formula C26H38O9
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SMILES
[H][C@@]12CC[C@](O)(C3)C(C[C@]31CC[C@@]4([C@](C)(C(O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)C(O)=O)O)O)O)=O)CCC[C@]42C)[H])=C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Steviol glucuronide
- 885044-59-7
- Drug Metabolite
- GCGR
- Free Radical Scavengers
- Insulin Receptor
- OAT
- Glucagon Receptor
- Organic anion transporter
- OAT3
- OATP1B1
- beta-2-microglobulin
- glucagon receptor
- glucose-dependent insulin secretion
- hydroxyl radicals
- pancreatic islets
- passive diffusion
- superoxide radicals
- type 2 diabetes
- Inhibitor
- inhibitor
- inhibit