AG 205

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Description: Progesterone receptor membrane component 1 (Pgrmc1) ligand
Chemical Name: cis-2-[[1-(4-Chlorophenyl)-1H-tetrazol-5-yl]thio]-1-(1,2,3,4,4a,9b-hexahydro-2,8-dimethyl-5H-pyrido[4,3-b]indol-5-yl)-ethanone
Purity: ≥97% (HPLC)
Datasheet
Citations (2)
Reviews

Biological Activity for AG 205

AG 205 is a progesterone receptor membrane component 1 (Pgrmc1) ligand. Inhibits cell cycle progression and cell viability in cancer cell lines. Inhibits progesterone induced cytosolic Ca2+ increases in GnRH neurons in vitro.

Technical Data for AG 205

M. Wt 454.98
Formula C22H23ClN6OS
Storage Store at +4°C
Purity ≥97% (HPLC)
CAS Number 442656-02-2
PubChem ID 4240652
InChI Key GJNBAISSZRNGTM-UHFFFAOYSA-N
Smiles [H][C@@]12CCN(C)C[C@]1([H])C1=CC(C)=CC=C1N2C(=O)CSC1=NN=NN1C1=CC=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AG 205

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.75 50

Preparing Stock Solutions for AG 205

The following data is based on the product molecular weight 454.98. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.4 mL 21.98 mL 43.96 mL
2.5 mM 0.88 mL 4.4 mL 8.79 mL
5 mM 0.44 mL 2.2 mL 4.4 mL
25 mM 0.09 mL 0.44 mL 0.88 mL

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References for AG 205

References are publications that support the biological activity of the product.

Ahmed et al (2010) Progesterone receptor membrane component 1 (Pgrmc1): a heme-1 domain protein that promotes tumorigenesis and is inhibited by a small molecule. J.Pharmacol.Exp.Ther. 333 564 PMID: 20164297

Bashour and Wray (2012) Progesterone directly and rapidly inhibits GnRH neuronal activity via progesterone receptor membrane component 1. Endocrinology. 153 4457 PMID: 22822163

Yoshitani et al (2005) A structure-based strategy for discovery of small ligands binding to functionally unknown proteins: combination of in silico screening and surface plasmon resonance measurements. Proteomics. 5 1472 PMID: 15798990


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Keywords: AG 205, AG 205 supplier, AG205, progesterone, receptor, membrane, component, 1, Pgrmc1, ligands, inhibitors, inhibits, Progesterone, Receptor, 6242, Tocris Bioscience

2 Citations for AG 205

Citations are publications that use Tocris products. Selected citations for AG 205 include:

Leena et al (2021) PGRMC1 acts as a size-selective cargo receptor to drive ER-phagic clearance of mutant prohormones. Nat Commun 12 5991 PMID: 34645803

Matthias et al (2021) The PGRMC1 Antagonist AG-205 Inhibits Synthesis of Galactosylceramide and Sulfatide. Cells 10 PMID: 34944026


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