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Cycloastragenol Telomerase activator

Name: Cycloastragenol
Brand: Selleck Chemicals
SKU: S3894
Rating: 5 (1 reviews)

Cat.No.S3894

Cycloastragenol (CAG, TA-65, Cyclogalegigenin, Astramembrangenin) is a saponin comprising a group of oil glucosides naturally present in a number of plants. It is a potent telomerase activator in neuronal cells.

Chemical Structure

Molecular Weight: 490.72

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Quality Control

Batch: Purity: 100.00%

100.00

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other Telomerase Inhibitors	EGCG ((-)-Epigallocatechin Gallate) BIBR 1532 Costunolide RHPS 4 methosulfate Cyclogalegenol Epitalon MST-312 L-778123 hydrochloride TAC (TERT Activator-1) Braco-19 trihydrochloride

Chemical Information, Storage & Stability

Molecular Weight	490.72	Formula	C₃₀H₅₀O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	84605-18-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CAG, TA-65, Cyclogalegigenin, Astramembrangenin			Smiles	CC1(C(CCC23C1C(CC4C2(C3)CCC5(C4(CC(C5C6(CCC(O6)C(C)(C)O)C)O)C)C)O)O)C

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (199.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	telomerase
In vitro	Cycloastragenol stimulates telomerase activity and cell proliferation in human neonatal keratinocytes. It induces telomerase activity and cAMP response element binding (CREB) activation in PC12 cells and primary neurons. This compound treatment not only induces the expression of bcl2, a CREB-regulated gene, but also the expression of telomerase reverse transcriptase in primary cortical neurons. It rapidly passes through the Caco-2 cell monolayer by passive diffusion. Once passage through the intestinal epithelium, first-pass intestinal metabolism of this chemical might occur. It can undergo extensive metabolism in rat and human liver microsomes.
In vivo	Oral administration of cycloastragenol (CA) for 7 days attenuates depression-like behaviour in experimental mice. Oral bioavailability of this compound is about 25.70% at 10 mg/kg. It is excreted through bile and faeces and eliminated predominantly by the kidney in rats. There might also exist an enterohepatic circulation of this chemical in rats. It could be metabolised widely in vivo in rats. For oral administration the mean T_max at 10 mg/kg, 20 mg/kg, and 40 mg/kg is 2.06±0.58 h, 1.48±0.36 h, and 2.35± 1.17 h. The t_1/2 is 5.23±1.55 h, 7.33±3.03 h, and 6.06± 3.42 h, respectively. The mean absorption time of this compound at 10 mg/kg is 5.70± 1.62 h; the poor absorption could be caused by the low solubility. The pharmacokinetic parameters show no significant differences among the groups of 10, 20, and 40 mg/kg except for C_max and AUC.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25095809/ [2] https://pubmed.ncbi.nlm.nih.gov/27412909/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05777083	Recruiting	ST Elevation Myocardial Infarction\|Electrocardiogram	Ewha Womans University Mokdong Hospital	January 1 2023	Not Applicable
NCT05578443	Recruiting	Alzheimer''s Disease	Fujian Medical University Union Hospital	October 1 2022	Phase 2
NCT05528744	Recruiting	Genetic Disease\|Chopra-Amiel-Gordon Syndrome\|CAGS\|ANKRD17	Boston Children''s Hospital	August 27 2022	--
NCT05533528	Recruiting	Periodontal Pocket\|Periodontal Diseases\|Periodontal Bone Loss	Universidad de Murcia	May 3 2022	Not Applicable
NCT05118009	Completed	Myocardial Infarction Acute	National Defense Medical Center Taiwan	May 1 2022	Not Applicable

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