SKI2496 is a potent and orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist (hGnRHR IC50 = 0.46 nM; max. LH inh. inh. (%, h)= 84%, 12h; LH inh. (24h) = 76%.). SKI2496 exhibited more selective antagonistic activity toward the human GnRH receptors over the GnRHRs in monkeys and rats, and SKI2496 also showed inhibitory effects on GnRH-mediated signaling pathways. Pharmacokinetic and pharmacodynamic evaluations of SKI2496 revealed improved bioavailability and superior gonadotropic suppression activity compared with Elagolix, the most clinically advanced compound. SKI2496 may represent a promising candidate for an orally available hormonal therapy.
MedKoo Cat#: 526975
Name: SKI2496
CAS#: 1308378-95-1
Chemical Formula: C35H36F7N5O5
Exact Mass: 739.2605
Molecular Weight: 739.69
Elemental Analysis: C, 56.83; H, 4.91; F, 17.98; N, 9.47; O, 10.81
The following data is based on the product molecular weight 739.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
