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Sufugolix

Catalog No. T3538 CAS 308831-61-0

Synonyms: TAK-013

TAK-013 is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor.

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Sufugolix, CAS 308831-61-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAK-013 is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor.
Targets&IC50	LHRH:0.1 nM.
In vitro	Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. It is observed that the cis conformer of the methoxyurea is more populated than the trans conformer by high-temperature molecular dynamics calculation during the conformational analysis of sufugolix[1].
In vivo	Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). Sufugolix has the apparent lipophilicity to allow increased membrane permeability and consequently improve its oral absorption in monkeys. The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively[1].
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].

Synonyms	TAK-013
Molecular Weight	667.73
Formula	C36H31F2N5O4S
CAS No.	308831-61-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 10mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Sasaki S, et al. 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. 2003 Jan 2;46(1):113-24.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-COVID-19 Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library

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Keywords

Sufugolix 308831-61-0 内分泌与激素 LHRH TAK 013 TAK-013 Inhibitor inhibit TAK013 inhibitor

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