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| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
Purity: ≥98%
Epelsiban (also known as GSK557296; GSK-557296) is a novel, potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor. It was initially developed by GSK for the treatment of premature ejaculation in men and then as an agent to enhance embryo or blastocyst implantation in women undergoing embryo or blastocyst transfer associated with in vitro fertilization. Later it was also investigated for use in the treatment of adenomyosis. Epelsiban shows >31000-fold selectivity over all three human vasopressin receptors hV1aR, hV2R, and hV1bR, with no significant P450 inhibition. Epelsiban has low levels of intrinsic clearance against the microsomes of four species, good bioavailability (55%) and comparable potency to atosiban in the rat, but is 100-fold more potent than the latter in vitro and was negative in the genotoxicity screens with a satisfactory oral safety profile in female rats.
| ln Vitro |
Epelsiban is a powerful oxytocin receptor that exhibits no discernible P450 inhibition. It has a pKi of 9.9 for the human oxytocin receptor and >31000-fold selectivity over all three human vasopressin receptors: hV1aR (pKi, <5.2), hV2R (pKi, <5.1), and hV1bR (pKi, 5.4)[1].
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| ln Vivo |
In rats, epelsiban's IC50 for the oxytocin receptor is 192 nM. Epelsiban exhibits good bioavailability (55%) and low levels of intrinsic clearance against the microsomes of rats, dogs, and cynomolgus monkeys. However, it fails genotoxicity assays and has an acceptable oral safety profile in female rats[1].
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| References |
[1]. Borthwick AD, et al. Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency. J Med Chem. 2012 Jan 26;55(2):783-96.
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| Molecular Formula |
C30H38N4O4
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|---|---|
| Molecular Weight |
518.64712
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| CAS # |
872599-83-2
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| Related CAS # |
872599-83-2;1159097-48-9 (besylate);
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| SMILES |
O=C(N1CCOCC1)[C@@H](C2=C(N=C(C)C=C2)C)N3[C@](C(N[C@H](C4CC5=CC=CC=C5C4)C3=O)=O)([H])[C@@H](C)CC
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9281 mL | 9.6404 mL | 19.2808 mL | |
| 5 mM | 0.3856 mL | 1.9281 mL | 3.8562 mL | |
| 10 mM | 0.1928 mL | 0.9640 mL | 1.9281 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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