L-368,899

Cat. No. M28530

All AbMole products are for research use only, cannot be used for human consumption.

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Quality Control & Documentation

Purity: ≥99.0%
COA
MSDS

Product Information

Biological Activity

L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.

Chemical Information

Molecular Weight	554.77
Formula	C26H42N4O5S2
CAS Number	148927-60-0
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.

References

[1] Aaron L Smith, et al. Bioorg Med Chem Lett. Carbon-11 N-methyl alkylation of L-368,899 and in vivo PET imaging investigations for neural oxytocin receptors

[2] G E Mann, et al. Domest Anim Endocrinol. Attenuation of PGF2alpha release in ewes infused with the oxytocin antagonist L-368,899

[3] K L Thompson, et al. Drug Metab Dispos. Pharmacokinetics and disposition of the oxytocin receptor antagonist L-368,899 in rats and dogs

[4] D J Pettibone, et al. Adv Exp Med Biol. Progress in the development of oxytocin antagonists for use in preterm labor

[5] P D Williams, et al. J Med Chem. 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)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm l䲧瘀Ỵ

Related Oxytocin Receptor Products
Cligosiban Cligosiban (PF-3274167) is a high-affinity, high oral bioavailability and good brain-penetrant nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
Oxytocin acetate Oxytocin acetate, a mammalian neurohypophysial hormone, is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
Carbetocin Carbetocin is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
L-368,899 hydrochloride L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC₅₀s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively.
Atosiban Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

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L-368,899

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