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L-368,899 

Cat. No. M28530
L-368,899  Structure
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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.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

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

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Keywords: L-368,899  supplier, Oxytocin Receptor, inhibitors, activators

 
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