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| Targets |
Ecdysteroid receptor (EcR) in insects, acting as an agonist. In mammals, the molecular target is not definitively established, but the primary anabolic effects are proposed to be mediated through a non-androgen receptor pathway, specifically activation of the PI3K/Akt/mTOR signaling pathway, potentially involving an estrogen receptor beta (ERbeta) interaction. It may also bind to the sigma-1 receptor (Sig1R) with weak affinity. Turkesterone does not bind to the androgen receptor, which distinguishes it from traditional anabolic steroids.
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| ln Vitro |
Turkesterone's capacity to remove [3H]ponA from the in vitro-expressed DmEcR/DmUSP receptor complex was assessed. In the BII bioassay, the EC50 is 0.8 μM, while the receptor assay yields a Ki value of 90 nM [1].
In vitro, turkesterone (1-100 uM) scavenges DPPH radicals in a cell-free assay (IC50 = 140.92 ug/mL) and is cytotoxic to HeLa cervical (IC50 = 75.2 ug/mL, ∼151 uM), HepG2 hepatic (IC50 = 63.01 ug/mL, ∼127 uM), and MCF-7 breast cancer cells (IC50 = 105.2 ug/mL, ∼212 uM). It binds to the ecdysteroid receptor from Chironomus tentans with a Kd of 0.491 uM and induces pupariation in several insect species (ED50 values: 10 ug/larvae in Galleria mellonella, 0.03 ug/larvae in Sarcophaga bullata, and 0.2 ug/larvae in D. vulpinus). It has been reported to stimulate protein synthesis in cultured C2C12 mouse myotubes, likely via PI3K/Akt/mTOR pathway activation. |
| ln Vivo |
In vivo, turkesterone decreases serum glucose levels and increases serum insulin and C-peptide levels in an alloxan-induced diabetic rat model when administered at a dose of 10 mg/kg (likely intraperitoneally or orally). It also prevents immobilization stress-induced stomach ulcers in mice (dose not specified). In animal studies (primarily rats), it has been reported to possess potent anabolic properties, sometimes rivaling those of certain synthetic steroids, including increased muscle mass and improved exercise performance. However, these results have not been consistently replicated in human clinical trials, and the anabolic effects in humans remain largely unsubstantiated. One preliminary human study showed no significant impact on muscle mass or body composition.
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| Enzyme Assay |
Non-cellular binding assays for insect ecdysteroid receptor: The receptor from Chironomus tentans (source unspecified) is incubated with tritiated ponasterone A ([3H]-PonA) as the radioligand, along with varying concentrations of unlabeled turkesterone (0.01-10 uM) in appropriate buffer conditions. After a 60-90 minute incubation, bound ligand is separated by filtration or a ligand-binding assay, and Kd values are calculated. For the DPPH radical scavenging assay, a 0.1 mM DPPH solution in methanol is mixed with turkesterone (12.5-200 ug/mL). After 30 minutes at room temperature, the absorbance is measured at 517 nm, and the IC50 is calculated.
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| Cell Assay |
C2C12 mouse myoblasts are differentiated into myotubes by culturing in DMEM with 2% horse serum for 5-7 days. Differentiated myotubes are then treated with turkesterone (1-100 uM) for 24-72 hours. Protein synthesis is assessed by [3H]-leucine incorporation or by measuring the incorporation of puromycin into newly synthesized proteins using an anti-puromycin antibody (SUnSET method). For signaling pathway analysis, cells are treated with turkesterone (10-100 uM) for 0-60 minutes, then lysed, and phosphorylated levels of Akt (Ser473), mTOR (Ser2448), p70S6K (Thr389), and 4E-BP1 (Thr37/46) are analyzed by western blot. Phospho-Akt activation can be blocked by the PI3K inhibitor LY294002, confirming pathway involvement.
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| Animal Protocol |
Alloxan-induced diabetic rat model: Male Wistar rats (180-200 g) are rendered diabetic by a single intraperitoneal injection of alloxan monohydrate (150 mg/kg). After 72 hours, rats with blood glucose levels >250 mg/dL are selected. Turkesterone is administered at a dose of 10 mg/kg (route unspecified, likely intraperitoneal or oral) for 14-21 days. Blood glucose levels are measured weekly using a glucometer, and serum insulin and C-peptide levels are measured by ELISA at the end of the study. Pancreatic tissue is collected for histopathological examination (hematoxylin and eosin staining). The compound significantly reduces blood glucose and increases insulin/C-peptide levels in diabetic rats, indicating a protective effect on pancreatic beta-cells.
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| ADME/Pharmacokinetics |
No detailed PK data have been reported. Turkesterone has a molecular weight of 496.63 g/mol, a LogP of approximately 0.5-1.0 (due to multiple hydroxyl groups), and is soluble in DMSO (100 mg/mL). It has poor oral bioavailability in humans due to extensive first-pass metabolism (glucuronidation and sulfation) and active efflux by P-glycoprotein (P-gp). The half-life is predicted to be short (2-4 hours), and Cmax is expected to be low after oral administration, which may explain why anabolic effects are more readily observed in insect models (where metabolism is different) than in mammals. It is highly hydrophilic, limiting passive membrane diffusion.
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| Toxicity/Toxicokinetics |
Cell culture cytotoxicity: Turkesterone shows moderate cytotoxicity in human cancer cell lines (HeLa, HepG2, MCF-7) with IC50 values ranging from 63-105 ug/mL (127-212 uM). It is considered relatively safe at lower concentrations (<50 uM) and has a low acute toxicity profile in rodent models (no reported LD50, but likely >2000 mg/kg oral). In human studies (preliminary), turkesterone at typical dietary supplement doses (250-1000 mg/day) appears to be well-tolerated with no significant adverse events reported, though long-term safety data are lacking. Potential side effects are mild and may include gastrointestinal discomfort (nausea, bloating), headache, and skin rash. Because it does not bind to the androgen receptor, turkesterone does not cause androgenic side effects such as acne, hair loss, or virilization.
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| References | |
| Additional Infomation |
Turkone is a steroidal compound. It has been reported in Paris polyphylla, Viola yedoensis, and other organisms with available data.
Turkesterone is a naturally occurring phytoecdysteroid, but it is not a clinically approved drug for any indication. It is marketed as a dietary supplement for athletic performance enhancement, muscle building, and recovery, based on animal data and anecdotal reports, despite the lack of rigorous human clinical evidence. The US FDA has not evaluated these claims. It is not approved for any therapeutic use in humans. Turkesterone is sometimes confused with ecdysterone (20-hydroxyecdysone), another phytoecdysteroid; the two have different potencies and spectra of activity. Its anabolic mechanism is androgen receptor-independent and likely involves the PI3K/Akt/mTOR pathway. It is available from chemical suppliers for research use and as a supplement ingredient, but product quality and purity vary. There is no approved IND (Investigational New Drug) application or NDA (New Drug Application). |
| Molecular Formula |
C27H44O8
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|---|---|
| Molecular Weight |
496.63346
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| Exact Mass |
496.303
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| CAS # |
41451-87-0
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| PubChem CID |
14376672
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
740.1±60.0 °C at 760 mmHg
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| Flash Point |
415.3±29.4 °C
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| Vapour Pressure |
0.0±5.5 mmHg at 25°C
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| Index of Refraction |
1.610
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| LogP |
-1.53
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
902
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@]12C[C@H]([C@H]3C(=CC(=O)[C@H]4[C@@]3(C[C@@H]([C@@H](C4)O)O)C)[C@@]1(CC[C@@H]2[C@](C)([C@@H](CCC(C)(C)O)O)O)O)O
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| InChi Key |
WSBAGDDNVWTLOM-XHZKDPLLSA-N
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| InChi Code |
InChI=1S/C27H44O8/c1-23(2,33)8-7-21(32)26(5,34)20-6-9-27(35)15-11-16(28)14-10-17(29)18(30)12-24(14,3)22(15)19(31)13-25(20,27)4/h11,14,17-22,29-35H,6-10,12-13H2,1-5H3/t14-,17+,18-,19+,20-,21+,22+,24-,25+,26+,27+/m0/s1
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| Chemical Name |
(2S,3R,5R,9R,10R,11R,13R,14S,17S)-2,3,11,14-tetrahydroxy-10,13-dimethyl-17-[(2R,3R)-2,3,6-trihydroxy-6-methylheptan-2-yl]-2,3,4,5,9,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-6-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~201.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0136 mL | 10.0679 mL | 20.1357 mL | |
| 5 mM | 0.4027 mL | 2.0136 mL | 4.0271 mL | |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0136 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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