| Bioactivity | L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR[1][2]. | ||||||||||||
| Target | Ki: 4.8 (oxytocin) | ||||||||||||
| In Vivo | L-372662 is an antagonist of oxytocin-induced uterine contractions in late gestation pregnant rhesus monkeys (AD50 = 36 micrograms/kg), oral bioavailability (F = 90% in dogs), and aqueous solubility (10 mg/mL). | ||||||||||||
| Name | L-372662 | ||||||||||||
| CAS | 162045-26-3 | ||||||||||||
| Formula | C33H38N4O6 | ||||||||||||
| Molar Mass | 586.68 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bell, I. M., Erb, J. M., Freidinger, R. M., Gallicchio, S. N., Guare, J. P., Guidotti, M. T., … Woyden, C. J. (1998). Development of Orally Active Oxytocin Antagonists: Studies on 1-(1-{4-[1-(2-Methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- metho [2]. Hawtin SR, et al. A Gly/Ala switch contributes to high affinity binding of benzoxazinone-based non-peptide oxytocin receptor antagonists. FEBS Lett. 2005;579(2):349-356. [3]. Williams PD, et al. Progress in the development of oxytocin antagonists for use in preterm labor. Adv Exp Med Biol. 1998;449:473-479. |