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L-372662

Names

[ CAS No. ]:
162045-26-3

[ Name ]:
L-372662

[Synonym ]:
L-372662
2H-3,1-Benzoxazin-2-one, 1,4-dihydro-1-[1-[2-methoxy-4-[[1-[(2-methyl-1-oxido-3-pyridinyl)methyl]-4-piperidinyl]oxy]benzoyl]-4-piperidinyl]-
1-{1-[2-Methoxy-4-({1-[(2-methyl-1-oxido-3-pyridinyl)methyl]-4-piperidinyl}oxy)benzoyl]-4-piperidinyl}-1,4-dihydro-2H-3,1-benzoxazin-2-one
1-{1-[2-methoxy-4-({1-[(2-methyl-1-oxidopyridin-3-yl)methyl]piperidin-4-yl}oxy)benzoyl]piperidin-4-yl}-1,4-dihydro-2H-3,1-benzoxazin-2-one
MFCD00936338

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor

[Target]

Ki: 4.8 (oxytocin)[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- methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and Related Pyridines. Journal of Medicinal Chemistry, 41(12), 2146–2163.

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
810.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C33H38N4O6

[ Molecular Weight ]:
586.68

[ Flash Point ]:
444.2±34.3 °C

[ Exact Mass ]:
586.279114

[ LogP ]:
2.07

[ Vapour Pressure ]:
0.0±2.9 mmHg at 25°C

[ Index of Refraction ]:
1.647

Related Compounds