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Sufugolix

CAT: 0013-GTR19162642-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19162642-01Size:200 mg
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Description
Sufugolix (TAK-013) is a highly potent and orally bioavailable non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor with binding and functional IC50 of 0.1 and 0.06 nM for human LHRH, respectively; completely suppresses plasma LH levels in castrated male cynomolgus monkeys at 30 mg/kg dose with sufficient duration of action (>24 h) (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. During the conformational analysis of sufugolix, using high-temperature molecular dynamics calculation, it is observed that the cis conformer of the methoxyurea is more populated than the trans conformer . (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) . 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.
CAS Number
308831-61-0
Product Name Alternative
TAK013 | TAK-013 | TAK 013
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (NOC) NC1=CC=C (C (S2) =C (CN (C) CC3=CC=CC=C3) C (C (N4C5=CC=CC=C5) =O) =C2N (CC6=C (F) C=CC=C6F) C4=O) C=C1
Molecular Formula
C36H31F2N5O4S
Molecular Weight
667.7242
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Urea, N-[4-[1-[ (2,6-difluorophenyl) methyl]-1,2,3,4-tetrahydro-5-[[methyl (phenylmethyl) amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy-

Alternative Products

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T3538-01Sufugolix
A20589-50Sufugolix 50mg
A20589-1Sufugolix 1mg
A20589-100Sufugolix 100mg
A20589-25Sufugolix 25mg
A20589-10Sufugolix 10mg
A20589-5Sufugolix 5mg
A20589-2Sufugolix 2mg

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