L-368,899 | Oxytocin receptor antagonist

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Chemical Structure : L-368,899

L-368,899 (L-368899)

Catalog No.: PC-24223Not For Human Use, Lab Use Only.

L-368,899 is a potent, selective orally bioavailable, non-peptide oxytocin receptor (OTR, OXTR) antagonist with IC50 of 8.9 nM (rat uterus), and 26 nM (human uterus).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

L-368,899 is a potent, selective orally bioavailable, non-peptide oxytocin receptor (OTR, OXTR) antagonist with IC50 of 8.9 nM (rat uterus), and 26 nM (human uterus).
L-368,899 inhibits OT-stimulated contractions of the isolated rat uterus (pA2 = 8.9) and in situ rat uterus (AD50 = 0.35 mg/kg after intravenous (i.v.) administration and 7.0 mg/kg after intraduodenal administration).

Physicochemical Properties

M.Wt	554.77
Formula	C26H42N4O5S2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S)-2-Amino-N-((1S,2S)-7,7-dimethyl-1-(((4-(o-tolyl)piperazin-1-yl)sulfonyl)methyl)bicyclo[2.2.1]heptan-2-yl)-4-(methylsulfonyl)butanamide

References

1. Williams PD, et al. J Med Chem. 1994 Mar 4;37(5):565-71.

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L-368,899 (L-368899)

Biological Activity

Physicochemical Properties

References

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