Barusiban (Synonyms: FE-200440)

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Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (K_i=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research.

For research use only. We do not sell to patients.

Barusiban Chemical Structure

CAS No. : 285571-64-4

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Description

In Vitro

Barusiban shows affinity for oxytocin receptor (K_i=0.8 nM) in COS cells expressed with oxytocin receptor^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Barusiban (intravenous injection; 50 or 150 μg/kg; once) treatment shows inhibition on OT-induced contractions^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pregnant cynomolgus monkeys injected with oxytocin (OT)^[2]
Dosage:	50 or 150 μg/kg
Administration:	Intravenous injection; 50 or 150 μg/kg; once
Result:	Reduced uterine contractions to baseline levels effectively. Reduced intrauterine pressure (IUP) from 6-7.5 kmm Hg•h to approximately 1 kmm Hg•h.

Clinical Trial

Molecular Weight

830.05

Formula

C₄₀H₆₃N₉O₈S

CAS No.

285571-64-4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Helmer H, et al. Barusiban, a selective oxytocin receptor antagonist: placental transfer in rabbit, monkey, and human†. Biol Reprod. 2020 Jun 23;103(1):135-143. [Content Brief]

[2]. Reinheimer TM, et al. Barusiban, a new highly potent and long-acting oxytocin antagonist: pharmacokinetic and pharmacodynamic comparison with atosiban in a cynomolgus monkey model of preterm labor. J Clin Endocrinol Metab. 2005 Apr;90(4):2275-81. [Content Brief]

[3]. Gimpl G, et al. Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin. Eur J Pharmacol. 2005 Mar 7;510(1-2):9-16. [Content Brief]

Barusiban Related Classifications

Endocrinology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Barusiban285571-64-4FE-200440FE200440FE 200440Oxytocin ReceptorOXTROT-induced contractionpreterm laborPTLin vitro fertilisationIVFinfertilityInhibitorinhibitorinhibit

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