Amarogentin

For research use only.

Catalog No.S1273 Synonyms: AG

Amarogentin Chemical Structure

CAS No. 21018-84-8

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

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Description

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

Targets
TAS2R1 [2]
()
TNF-α [2]
()
AMPK [4]
()

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (170.49 mM)
Water Insoluble
Ethanol '''50 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 586.54
Formula

C29H30O13

CAS No. 21018-84-8
Storage powder
in solvent
Synonyms AG

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04759339 Completed Drug: AG-920 Healthy American Genomics LLC February 24 2021 Phase 1
NCT04145128 Completed Drug: AG881 Healthy Volunteers Agios Pharmaceuticals Inc. October 2 2019 Phase 1
NCT03834584 Terminated Drug: AG-636 Lymphoma Agios Pharmaceuticals Inc. May 24 2019 Phase 1
NCT03860935 Active not recruiting Drug: AG10|Drug: Placebo Oral Tablet Amyloidosis|Amyloid Cardiomyopathy|Transthyretin Amyloidosis|Cardiomyopathies|Heart Diseases Eidos Therapeutics March 19 2019 Phase 3
NCT03536767 Enrolling by invitation Drug: AG10 Amyloid Cardiomyopathy Eidos Therapeutics August 8 2018 Phase 2
NCT03234465 Terminated Biological: AG013|Other: Placebo Oral Mucositis Oragenics Inc. July 18 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID