| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Cycloastragenol functions as a telomerase activator. Telomerase is an enzyme that maintains telomere length, which is crucial for cellular longevity and replicative capacity. By activating telomerase, cycloastragenol can retard telomere shortening, increase proliferative potential, and enhance cellular function. The compound also increases phosphorylation of ERK, which may be dependent on Src and MEK signaling. Additionally, cycloastragenol exhibits anti-inflammatory and anti-oxidative properties.
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| ln Vitro |
Cycloastragenol has demonstrated significant in vitro activity in various cellular models. In CD8+ T lymphocytes from HIV-infected donors, it retarded telomere shortening, increased proliferative potential, and enhanced cytokine/chemokine production and antiviral activity. The compound has been shown to extend T cell proliferation by increasing telomerase activity. It also inhibits the apoptosis of PC12 cells induced by 6-OHDA, suggesting potential neuroprotective properties. Cycloastragenol activates telomerase ex vivo, preventing the development of fibrosis and increasing epithelial life span.
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| ln Vivo |
Cycloastragenol has demonstrated in vivo activity in animal models and is being investigated as a potential treatment for pulmonary fibrosis and other telomerase-associated disorders. The compound activates telomerase in vivo. It has been shown to have anti-inflammatory and anti-oxidative properties, as well as the ability to improve lipid metabolism. Cycloastragenol's potential neuroprotective effects have also been explored in the context of Parkinson's disease.
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| Enzyme Assay |
Cycloastragenol's activity as a telomerase activator is typically assessed using in vitro telomerase activity assays, such as the TRAP (Telomeric Repeat Amplification Protocol) assay. These assays measure the ability of the compound to enhance telomerase enzymatic activity. Binding studies may also be conducted to understand the compound's interaction with telomerase or other cellular targets. The compound's anti-inflammatory and anti-oxidative properties can be evaluated using standard biochemical assays.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HEK Cell Tested Concentrations: 1 µM, 3 µM, 10 µM Incubation Duration: 3-6 Days Experimental Results: Cell growth doubled at 6 days. Western Blot Analysis[2] Cell Types: Neuronal Cells Tested Concentrations: 0-3 µM Incubation Duration: 5 min, 15 min, 30 min, 90 min Experimental Results: Shows that CAG induces CREB activation in neuronal cells. Western Blot Analysis[2] Cell Types: Neuronal Cell Tested Concentrations: 0-3 µM Incubation Duration: 6-48 hrs (hours) Experimental Results: Increased expression of tert, bcl2 mRNA. Cellular assays for cycloastragenol involve treating cells with the compound and measuring telomerase activity, telomere length, and cell proliferation. In CD8+ T lymphocytes, the compound's effects on telomere shortening, proliferative potential, and cytokine/chemokine production have been evaluated. The compound's ability to inhibit apoptosis has been assessed in PC12 cells. Its effects on fibrosis and epithelial life span have also been studied in cellular models. |
| Animal Protocol |
In vivo animal model protocols for cycloastragenol involve its administration to animal models to study its effects on telomerase activation, fibrosis, and other disease conditions. The compound is being investigated as a potential treatment for pulmonary fibrosis and other telomerase-associated disorders. Studies may also evaluate its effects on lipid metabolism, inflammation, and oxidative stress. The compound's pharmacokinetic properties, including intestinal absorption and metabolism, have been studied.
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| ADME/Pharmacokinetics |
Cycloastragenol's pharmacokinetic properties have been studied, including in vitro intestinal absorption and first-pass intestinal and hepatic metabolism. As a small molecule terpenoid, it is expected to have reasonable oral bioavailability. The compound is well-absorbed and undergoes metabolism in the intestine and liver. Specific pharmacokinetic parameters such as half-life and clearance would need to be determined in animal models.
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| Toxicity/Toxicokinetics |
Specific toxicological data for cycloastragenol is not extensively detailed in the available literature. As a natural product derived from Astragalus, it is generally considered to have a favorable safety profile. However, comprehensive toxicology studies would be required for clinical development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Cycloastragenol is a saponin, a derivative of astragaloside IV, the main saponin extracted from the root of Astragalus membranaceus. It is a metabolite. It is a saponin belonging to the pentacyclic triterpenoids, tetraols, and oxacyclopentanes. It is derived from the hydride of 5α-pyrene. Cycloastragenol has been reported to exist in Astragalus microcephalus, Astragalus coluteocarpus, and other organisms with relevant data.
Cycloastragenol (CAS# 84605-18-5) is a novel naturally occurring terpenoid found in Astragalus species. It is the aglycone derivative of astragaloside IV and has been shown to be a telomerase activator. The compound has a molecular formula of C30H50O5 and a molecular weight of 490.73. Extensive pharmacological effects have been attributed to cycloastragenol, including telomerase activation, telomere elongation, anti-inflammatory and anti-oxidative properties, improvement of lipid metabolism, and wound repair promotion. It is being investigated as a potential treatment for pulmonary fibrosis, Parkinson's disease, and other telomerase-associated disorders. |
| Molecular Formula |
C30H50O5
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|---|---|
| Molecular Weight |
490.72
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| Exact Mass |
490.365
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| CAS # |
84605-18-5
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| Related CAS # |
Cycloastragenol;78574-94-4
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| PubChem CID |
13943286
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
617.2±55.0 °C at 760 mmHg
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| Flash Point |
327.1±31.5 °C
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| Vapour Pressure |
0.0±4.0 mmHg at 25°C
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| Index of Refraction |
1.582
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| LogP |
3.82
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
35
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| Complexity |
916
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@]12CC[C@@]34C[C@@]35CC[C@@H](C([C@@H]5[C@H](C[C@H]4[C@@]1(C[C@@H]([C@@H]2[C@]6(CC[C@H](O6)C(C)(C)O)C)O)C)O)(C)C)O
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| InChi Key |
WENNXORDXYGDTP-UOUCMYEWSA-N
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| InChi Code |
InChI=1S/C30H50O5/c1-24(2)20(33)8-11-30-16-29(30)13-12-26(5)23(28(7)10-9-21(35-28)25(3,4)34)18(32)15-27(26,6)19(29)14-17(31)22(24)30/h17-23,31-34H,8-16H2,1-7H3/t17-,18-,19-,20-,21-,22-,23-,26+,27-,28+,29-,30+/m0/s1
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| Chemical Name |
(1S,3R,6S,8R,9S,11S,12S,14S,15R,16R)-15-[(2R,5S)-5-(2-hydroxypropan-2-yl)-2-methyloxolan-2-yl]-7,7,12,16-tetramethylpentacyclo[9.7.0.01,3.03,8.012,16]octadecane-6,9,14-triol
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| Synonyms |
Astramembrangenin; Cyclogalegigenin
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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 |
| 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 (~203.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0378 mL | 10.1891 mL | 20.3782 mL | |
| 5 mM | 0.4076 mL | 2.0378 mL | 4.0756 mL | |
| 10 mM | 0.2038 mL | 1.0189 mL | 2.0378 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02530255
Conditions:Alzheimer DiseaseProducts are for research use only; We do not sell to patients
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