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BAY-784, (2S)-N-[[3-Chloro-5-(trifluoromethyl)-2-pyridyl]methyl]-2-cyclopropyl-1-(4-fluorophenyl)sulfonyl-1′,1′-dioxo-spiro[indoline-3,4′-thiane]-5-carboxamide, (2S)-N-[[3-chloro-5-(trifluoromethyl)-2-pyridinyl]methyl]-2-cyclopropyl-1-[(4-fluorophenyl)sulfonyl]-1,2,2?,3?,5?,6?-hexahydro-spiro[3H-indole-3,4?-[4H]thiopyran]-5-carboxamide 1?,1?-dioxide, BAY 1214784, BAY-1214784
C29H26ClF4N3O5S2
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Quality Level
Assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -120 to -100°, c = 0.5 in chloroform-d
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=S(CCC1(C2=C(N3S(C4=CC=C(F)C=C4)(=O)=O)C=CC(C(NCC5=C(Cl)C=C(C(F)(F)F)C=N5)=O)=C2)[C@@H]3C6CC6)(CC1)=O
Biochem/physiol Actions
BAY-784 is an orally available, non-toxic, potent, and selective antagonist of human Gonadotropin-Releasing Hormone Receptor [hGnRH-R], which is potently active in other species including rate, dogs and cynomolgus monkey. It partially lowered plasma luteinizing hormone levels in humans. BAY-784 exhibits favorable drug metabolism and pharmacokinetic (DMPK) profile thus is suitable for in vivo studies.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Journal of medicinal chemistry, 63(20), 11854-11881 (2020-09-23)
The growth of uterine fibroids is sex hormone-dependent and commonly associated with highly incapacitating symptoms. Most treatment options consist of the control of these hormonal effects, ultimately blocking proliferative estrogen signaling (i.e., oral contraceptives/antagonization of human gonadotropin-releasing hormone receptor [hGnRH-R]
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