SUFUGOLIX
- Product Name
- SUFUGOLIX
- CAS No.
- 308831-61-0
- Chemical Name
- SUFUGOLIX
- Synonyms
- TAK013;SUFUGOLIX;tak-013, >98%;TAK013;TAK 013;SUFUGOLIX, >98%;Sufugolix(TAK-013);Sufugolix, 10 mM in DMSO;TAK 013,Inhibitor,Sufugolix,inhibit,TAK013;N-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-1,2,3,4-tetrahydro-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea;TAK-013 1-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
- CBNumber
- CB12451333
- Molecular Formula
- C36H31F2N5O4S
- Formula Weight
- 667.72
- MOL File
- 308831-61-0.mol
SUFUGOLIX Property
- Density
- 1.383±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C,unstable in solution, ready to use.
- solubility
- DMF: 5mg/mL; DMF:PBS (pH 7.2) (1:2): 0.3mg/mL; DMSO: 3mg/mL
- form
- A solid
- pka
- 13.20±0.70(Predicted)
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 27996
- Product name
- Sufugolix
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
- Product number
- 27996
- Product name
- Sufugolix
- Packaging
- 10mg
- Price
- $223
- Updated
- 2024/03/01
- Product number
- 27996
- Product name
- Sufugolix
- Packaging
- 5mg
- Price
- $145
- Updated
- 2024/03/01
- Product number
- 6280CJ
- Product name
- Sufugolix
- Packaging
- 5mg
- Price
- $260
- Updated
- 2021/12/16
- Product number
- BRS0000770
- Product name
- TAK-013
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $943.91
- Updated
- 2021/12/16
SUFUGOLIX Chemical Properties,Usage,Production
Description
Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 0.1 nM). Sufugolix inhibits GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor. It inhibits luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells ex vivo (IC50 = 36 nM). Sufugolix (10 and 30 mg/kg) reduces increases in plasma LH following castration in male cynomolgus monkeys and lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a dose of 90 mg/kg.
Uses
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
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[1].
References
[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. DOI:10.1021/jm020180i