Product Name :
Sufugolix
Description:
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
CAS:
308831-61-0
Molecular Weight:
667.72
Formula:
C36H31F2N5O4S
Chemical Name:
1-[4-(5-{[benzyl(methyl)amino]methyl}-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenyl-1H,2H,3H,4H-thieno[2,3-d]pyrimidin-6-yl)phenyl]-3-methoxyurea
Smiles :
CN(CC1=C(SC2=C1C(=O)N(C1C=CC=CC=1)C(=O)N2CC1C(F)=CC=CC=1F)C1C=CC(=CC=1)NC(=O)NOC)CC1C=CC=CC=1
InChiKey:
UCQSBGOFELXYIN-UHFFFAOYSA-N
InChi :
InChI=1S/C36H31F2N5O4S/c1-41(20-23-10-5-3-6-11-23)21-28-31-33(44)43(26-12-7-4-8-13-26)36(46)42(22-27-29(37)14-9-15-30(27)38)34(31)48-32(28)24-16-18-25(19-17-24)39-35(45)40-47-2/h3-19H,20-22H2,1-2H3,(H2,39,40,45)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Eptinezumab} site|{Eptinezumab} GPCR/G Protein|{Eptinezumab} Purity & Documentation|{Eptinezumab} References|{Eptinezumab} manufacturer|{Eptinezumab} Autophagy}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.|Product information|CAS Number: 308831-61-0|Molecular Weight: 667.72|Formula: C36H31F2N5O4S|Chemical Name: 1-[4-(5-{[benzyl(methyl)amino]methyl}-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenyl-1H,2H,3H,4H-thieno[2,3-d]pyrimidin-6-yl)phenyl]-3-methoxyurea|Smiles: CN(CC1=C(SC2=C1C(=O)N(C1C=CC=CC=1)C(=O)N2CC1C(F)=CC=CC=1F)C1C=CC(=CC=1)NC(=O)NOC)CC1C=CC=CC=1|InChiKey: UCQSBGOFELXYIN-UHFFFAOYSA-N|InChi: InChI=1S/C36H31F2N5O4S/c1-41(20-23-10-5-3-6-11-23)21-28-31-33(44)43(26-12-7-4-8-13-26)36(46)42(22-27-29(37)14-9-15-30(27)38)34(31)48-32(28)24-16-18-25(19-17-24)39-35(45)40-47-2/h3-19H,20-22H2,1-2H3,(H2,39,40,45)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 1.{{Gantenerumab} web|{Gantenerumab} Neuronal Signaling|{Gantenerumab} Biological Activity|{Gantenerumab} Description|{Gantenerumab} manufacturer|{Gantenerumab} Epigenetic Reader Domain} 25 mg/mL (1.PMID:25105126 87 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.|Products are for research use only. Not for human use.|
