Product Details
| Product Name:
Sufugolix |
CAS No.:
308831-61-0 |
| Purity:
95.06% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Sufugolix |
| Description | Sufugolix (TAK-013) is a potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist. |
| Kinase Assay | The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1]. |
| In vitro | Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. It effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. High-temperature molecular dynamics calculation during the conformational analysis of sufugolix reveals that the cis conformer of the methoxyurea is more populated than the trans conformer[1]. |
| In vivo | Oral administration of sufugolix at a 30 mg/kg dose causes almost complete suppression of plasma LH levels in castrated male cynomolgus monkeys for more than 24 hours. Sufugolix exhibits sufficient lipophilicity for enhanced membrane permeability and improved oral absorption in monkeys. Maximum plasma concentrations are 0.34 μM (6 hours post-administration) and 0.18 μM (4 hours post-administration) at 30 and 10 mg/kg doses, respectively[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 25 mg/mL (37.44 mM)
|
| Keywords | Inhibitor | TAK013 | Sufugolix | TAK 013 | inhibit |
| Inhibitors Related | Antide acetate |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States