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Amarogentin Taste Receptor agonist

Name: Amarogentin
Brand: Selleck Chemicals
SKU: S1273
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1273

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. This compound is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. It induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. This chemical interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

Chemical Structure

Molecular Weight: 586.54

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Quality Control

Batch: S127301 DMSO]100 mg/mL]false]Ethanol]50 mg/mL]false]Water]Insoluble]false Purity: 99.17%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.17

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Taste Receptor Inhibitors	Perillartine Aspartame

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (170.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (8.52mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Chemical Information, Storage & Stability

Molecular Weight	586.54	Formula	C₂₉H₃₀O₁₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	21018-84-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AG			Smiles	OCC1OC(OC2OC=C3C(CCOC3=O)C2C=C)C(OC(=O)C4=C(O)C=C(O)C=C4C5=CC=CC(=C5)O)C(O)C1O

Mechanism of Action

Targets/IC₅₀/Ki	TAS2R1 TNF-α AMPK
References	[1] https://pubmed.ncbi.nlm.nih.gov/28481234/ [2] https://pubmed.ncbi.nlm.nih.gov/26600671/ [3] https://pubmed.ncbi.nlm.nih.gov/27569081/ [4] https://pubmed.ncbi.nlm.nih.gov/31125678/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06298474	Not yet recruiting	Dementia\|Alzheimer Disease\|Vascular Dementia	Hopeful Aging	February 15 2025	Not Applicable
NCT06045988	Not yet recruiting	Alzheimer Disease\|Dementia\|Sleep Disturbance	Indiana University\|Innovative Design Labs\|University of Minnesota\|Mayo Clinic\|Regenstrief Institute Inc.\|National Institute on Aging (NIA)	February 1 2025	Phase 2
NCT06117176	Not yet recruiting	Airway Complication of Anesthesia\|Adverse Events	Insel Gruppe AG University Hospital Bern\|University of Bern\|University of Lausanne Hospitals\|Kantonsspital Aarau\|Charite University Berlin Germany\|Universitätsklinikum Hamburg-Eppendorf	January 2025	--
NCT05940766	Not yet recruiting	Pediatric Oncology Patients With Risk for Infections	Insel Gruppe AG University Hospital Bern\|ETH Zurich	October 1 2024	Not Applicable
NCT06370572	Not yet recruiting	Dementia\|Hip Pain\|Emergency Department Patient\|Pain in Advanced Dementia Scale	University of Chicago\|National Institute on Aging (NIA)\|University of North Carolina Chapel Hill	August 2024	Not Applicable
NCT05457725	Not yet recruiting	Neurocognitive Disorders\|Aging\|Cognitive Change	University of Florida\|National Institute on Aging (NIA)	July 1 2024	Early Phase 1

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