| Identification | Back Directory | [Name]
L 372662 | [CAS]
162045-26-3 | [Synonyms]
L 372662
3-((4-(3-METHOXY-4-(4-(2-OXO-2H-BENZO[D][1,3]OXAZIN-1(4H)-YL)PIPERIDINE-1-CARBONYL)PHENOXY)PIPERIDIN-1-YL)METHYL)-2-METHYLPYRIDINE 1-OXIDE | [Molecular Formula]
C33H38N4O6 | [MDL Number]
MFCD00936338 | [MOL File]
162045-26-3.mol | [Molecular Weight]
586.68 |
| Chemical Properties | Back Directory | [Boiling point ]
810.8±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
6.35±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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). | [References]
[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. DOI:10.1016/j.febslet.2004.10.108
[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. DOI:10.1007/978-1-4615-4871-3_61 |
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| Company Name: |
AstaTech, Inc
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| Tel: |
(215) 785 3197 |
| Website: |
www.astatechinc.com |
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