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TGR5 Receptor Agonist

Catalog No. T1824 CAS 1197300-24-5

TGR5 is a potent TGR5(GPCR19) agonist.

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TGR5 Receptor Agonist Chemical Structure

TGR5 Receptor Agonist, CAS 1197300-24-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 79.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 483.00
100 mg	In stock	$ 693.00
1 mL * 10 mM (in DMSO)	In stock	$ 88.00

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Purity: 99.93%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TGR5 is a potent TGR5(GPCR19) agonist.
Targets&IC50	TGR5/GPCR19 (U2-OS cells):6.8(pEC50), TGR5/GPCR19 (melanophore cells):7.5(pEC50)
Kinase Assay	Inhibition assays are carried out in 384-well white ProxiPlates in 10 μL of reaction volume. Standard reaction mixtures consisted of the compound (in 2% DMSO final concentration), enzyme mix (0.001 μM of PHD2, 10 μM of Fe(II), 100 μM of ascorbate) and peptide mix (0.06 μM of biotinylated C-terminal oxygen dependent degradation domain (CODD) peptide, 2 μM of 2OG) in 50 mM HEPES pH 7.5, 0.01% Tween-20 and 0.1% BSA buffer. Compounds (e.g., IOX2) are preincubated with the enzyme mix for 15 min before being incubated with peptide mix for 10 min at 22°C. Each reaction is quenched with 5 μL of 30 mM EDTA. The bead mix containing AlphaScreen beads is preincubated for 1h with a rabbit monoclonal antibody selective for hydroxy-HIF1α (Pro564) and are added to the wells for a further 1 h at 22°C. The plates are then analyzed with an Envision plate reader. The IC50 values are calculated using nonlinear regression with normalized dose-response fit using Prism GraphPad (n≥3)[1].

Molecular Weight	361.22
Formula	C18H14Cl2N2O2
CAS No.	1197300-24-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mM

Ethanol: 100 mM

References and Literature

1. Evans KA, et al. J Med Chem. 2009 Dec 24;52(24): 7962-5.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Cancer Compound Library Anti-Obesity Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TGR5 Receptor Agonist 1197300-24-5 GPCR/G Protein GPCR19 Calcium Channel anti-obesity Inhibitor bladder hypersensitivity TGR5 G-protein coupled receptor 19 GPBAR1 U2-OS cells C57BL/6J mice G protein-coupled Bile Acid Receptor 1 melanophore cells Ca2+ channels inhibit TGR-5 Receptor Agonist diabetes TGR5 Receptor Agonist CCDC Ca channels inhibitor

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