L-368899 | Peptides (Hypothalamic / Pituitary Hormones) | Potent, Non-peptide Oxytocin Receptor Antagonist | L368899

Category:

Peptides (Hypothalamic/Pituitary Hormones)

Cat.No.	Product Name
2641	L-368,899 hydrochloride

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L-368899

Chemical Name: (2S)-2-Amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methy lphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]he pt-2-yl]-4-(methylsulfonyl)butanamide

Biological Activity:

Potent, non-peptide and orally active oxytocin receptor antagonist (IC₅₀ = 8.9 nM) that displays > 40-fold selectivity over vasopressin V_1a and V₂ receptors (IC₅₀ values are 370 and 570 nM respectively). Antagonises oxytocin-induced uterine contractions in vitro and in vivo.

Technical Data:

M.Wt:	591.23
Formula:	C₂₆H₄₂N₄O₅S₂.HCl
Storage:	Store at +4°C
Solubility:	Soluble to 100 mM in Water
Purity:	>99%
CAS No:	[148927-60-0]

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Certificate of Analysis / MSDS:

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References:

Williams et al (1994) 1-(((7,7-dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. J.Med.Chem. 37 565. Mann et al (2003) Attenuation of PGE₂_α release in ewes infused with the oxytocin antagonist L-368,899. Domest.Anim.Endocrinol. 25 255. Quattropani et al (2005) Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonist. J.Med.Chem. 48 7882.

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Keywords: L-368899, Peptides (Hypothalamic / Pituitary Hormones), Potent, Non-peptide Oxytocin Receptor Antagonist, L368899, Tocris Bioscience

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