T 98475

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Cat.No. 2519 - T 98475 | C37H37F2N3O4S | CAS No. 199119-18-1
Description: GnRH receptor antagonist
Chemical Name: 7-[(2,6-Difluorophenyl)methyl]-4,7-dihydro-2-[4-[(2-methyl-1-oxopropyl)amino]phenyl]-3-[[methyl(phenylmethyl)amino]methyl]-4-oxo-thieno[2,3-b]pyridine-5-carboxylic acid 1-methylethyl ester
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

Potent, orally active and non-peptide gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist (IC50 values are 0.2, 4.0 and 60 nM for human, monkey and rat GnRH receptors respectively). Inhibits LH release in vitro (IC50 = 100 nM) and reduces plasma LH concentration in castrated male cynomolgus monkeys.

Technical Data

M. Wt 657.77
Formula C37H37F2N3O4S
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 199119-18-1
PubChem ID 9874838
InChI Key RANJJVIMTOIWIN-UHFFFAOYSA-N
Smiles CC(C)OC(=O)C1=CN(CC2=C(F)C=CC=C2F)C2=C(C(CN(C)CC3=CC=CC=C3)=C(S2)C2=CC=C(NC(=O)C(C)C)C=C2)C1=O

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 32.89 50

Preparing Stock Solutions

The following data is based on the product molecular weight 657.77. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.04 mL 15.2 mL 30.41 mL
2.5 mM 0.61 mL 3.04 mL 6.08 mL
5 mM 0.3 mL 1.52 mL 3.04 mL
25 mM 0.06 mL 0.3 mL 0.61 mL

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References

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

Cho et al (1998) Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J.Med.Chem. 41 4190 PMID: 9784092

Sasaki et al (2003) Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J.Med.Chem. 46 113 PMID: 12502365

Imada et al (2006) Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. J.Med.Chem. 49 3809 PMID: 16789738


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