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| Size | Price | Stock |
|---|---|---|
| 5mg | $135 | To Be Confirmed |
| 10mg | $200 | To Be Confirmed |
| 25mg | $340 | To Be Confirmed |
| 50mg | $510 | To Be Confirmed |
| 100mg | $769 | To Be Confirmed |
| 250mg | $1340 | To Be Confirmed |
| 500mg | $1950 | To Be Confirmed |
: Cat #: V4597 CAS #: 308831-61-0 Purity ≥ 98%
Description: Sufugolix (formerly known as TAK-013) is a novel, highly potent, non-peptide, selective and orally bioavailable luteinizing hormone-releasing hormone (LHRH) receptor antagonist with anticancer activity. It inhibits LHRH with an IC50 of 0.1 nM. Sufugolix was under development for the treatment of endometriosis and uterine leiomyoma and reached phase II clinical trials for both of these indications, but was discontinued.
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| CAS No. | 308831-61-0 |
|---|---|
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent |
| Protocol | 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 [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). 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]. |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.