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Cycloastragenol

Cat No.:V17287 Purity: ≥98%
Cycloastragenol (Astramembrangenin) is the active form of astragaloside IV and has antioxidant, anti~inflammatory, anti-aging, anti-apoptotic and cardiovascular protective effects.
Cycloastragenol
Cycloastragenol Chemical Structure CAS No.: 78574-94-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Cycloastragenol:

  • Cycloastragenol
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Top Publications Citing lnvivochem Products
Product Description
Cycloastragenol (Astramembrangenin) is the active form of astragaloside IV and has antioxidant, anti~inflammatory, anti-aging, anti-apoptotic and cardiovascular protective effects. Cycloastragenol is a potent telomerase activator that can lengthen telomeres. Cycloastragenol alleviates age-related bone loss and improves bone microarchitecture and biomechanical properties.
Cycloastragenol (CAS#: 78574-94-4), also known as Astramembrangenin, is a potent telomerase activator that can lengthen telomeres. It has the molecular formula C30H50O5 and a molecular weight of 490.72. Cycloastragenol is the active form of astragaloside IV and has antioxidant, anti-inflammatory, anti-aging, anti-apoptotic, and cardiovascular protective effects. It alleviates age-related bone loss and improves bone microstructure and biomechanical properties. The compound upregulates SIRT1 expression, attenuates apoptosis, and suppresses the mRNA expression of pro-inflammatory cytokines including TNF-α and IL-1β.
Biological Activity I Assay Protocols (From Reference)
Targets
Telomerase. Cycloastragenol is a potent telomerase activator that can lengthen telomeres. It upregulates SIRT1 expression and suppresses the mRNA expression of pro-inflammatory cytokines including TNF-α and IL-1β. The compound has antioxidant, anti-inflammatory, anti-aging, anti-apoptotic, and cardiovascular protective effects.
ln Vitro
MC3T3-E1 cells' viability, osteoblast differentiation, and mineralization can all be enhanced by cycloastraganol (0.03-3 μM; 24-72 hours) [3].
Cycloastragenol activates telomerase, helping maintain telomere length and promote cellular longevity. It alleviates age-related bone loss and improves bone microstructure and biomechanical properties. The compound upregulates SIRT1 expression, attenuates apoptosis, and suppresses the mRNA expression of pro-inflammatory cytokines including TNF-α and IL-1β. It exhibits antioxidant, anti-inflammatory, and neuroprotective activities.
ln Vivo
Intraperitoneal injections of cycloastragenol (5, 10, 20 mg/kg) were given at the start of reperfusion, 12 hours later, and then twice a day for the next three days. In mice with middle cerebral artery occlusion (MCAO), cycloastragenol dose-dependently decreases the amount of the cerebral infarct, greatly improves functional impairments, and stops the loss of neuronal cells. Cycloastraganol suppresses the activation of microglia and astrocytes in the ischemic brain as well as the mRNA expression of pro-inflammatory cytokines such as TNF-α and IL-1β [2].
In vivo, cycloastragenol alleviates age-related bone loss and improves bone microstructure and biomechanical properties. It suppresses the mRNA expression of pro-inflammatory cytokines and inhibits the activation of microglia and astrocytes in the ischemic brain. The compound has anti-aging effects and can be used in cosmetic materials.
Enzyme Assay
In vitro enzyme assays for cycloastragenol involve measuring its activation of telomerase activity. Telomerase is incubated with its substrate and various concentrations of cycloastragenol. Telomerase activity is measured using the TRAP (telomeric repeat amplification protocol) assay. The compound's ability to activate telomerase is assessed.
Cell Assay
In vitro cellular assays for cycloastragenol involve treating cells (such as keratinocytes or neuronal cells) with the compound and measuring telomerase activity, telomere length, cell proliferation, or apoptosis. Cells are treated with various concentrations of cycloastragenol, and telomerase activity is measured by TRAP assay. Telomere length is measured by qPCR or Southern blot. Cell viability and apoptosis are assessed by MTT and flow cytometry.
Animal Protocol
In vivo animal studies for cycloastragenol typically involve administration to rodent models of aging, bone loss, or ischemia. Efficacy is assessed by measuring bone density, microstructure, biomechanical properties, or neurological function. Cycloastragenol alleviates age-related bone loss and improves bone microstructure and biomechanical properties.
ADME/Pharmacokinetics
Cycloastragenol has a molecular weight of 490.72 and a molecular formula of C30H50O5. It is the active form of astragaloside IV. The compound activates telomerase and can lengthen telomeres. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and elimination.
Toxicity/Toxicokinetics
Preclinical toxicity studies of cycloastragenol are limited. The compound has antioxidant, anti-inflammatory, anti-aging, anti-apoptotic, and cardiovascular protective effects. It alleviates age-related bone loss. Comprehensive toxicological evaluation is needed before clinical development. The compound should be handled with appropriate safety precautions.
References

[1]. Cycloastragenol: An exciting novel candidate for age-associated diseases. Exp Ther Med. 2018;16(3):2175-2182.

[2]. Cycloastragenol upregulates SIRT1 expression, attenuates apoptosis and suppresses neuroinflammation after brain ischemia. Acta Pharmacol Sin. 2020;41(8):1025-1032.

[3]. Cycloastragenol prevents age-related bone loss: Evidence in d-galactose-treated and aged rats. Biomed Pharmacother. 2020;128:110304.

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 (Astramembrangenin) is a potent telomerase activator that can lengthen telomeres. It is the active form of astragaloside IV and has antioxidant, anti-inflammatory, anti-aging, anti-apoptotic, and cardiovascular protective effects. Cycloastragenol alleviates age-related bone loss, improves bone microstructure, upregulates SIRT1 expression, and suppresses pro-inflammatory cytokine expression. It is a valuable natural compound for aging and bone health research.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H50O5
Molecular Weight
490.7150
Exact Mass
490.365
CAS #
78574-94-4
Related CAS #
Cyclogalegenin;84605-18-5
PubChem CID
13943286
Appearance
White to off-white solid powder
Density
1.2±0.1 g/cm3
Boiling Point
617.2±55.0 °C at 760 mmHg
Melting Point
241.0 to 245.0 °C
Flash Point
327.1±31.5 °C
Vapour Pressure
0.0±4.0 mmHg at 25°C
Index of Refraction
1.582
LogP
3.82
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
2
Heavy Atom Count
35
Complexity
916
Defined Atom Stereocenter Count
12
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
InChi Key
WENNXORDXYGDTP-UOUCMYEWSA-N
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
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
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~66.67 mg/mL (~135.86 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.09 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.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.24 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 20.8 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.24 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 20.8 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.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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