Barusiban
Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=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.
- CAS No.: 285571-64-4
- Formula: C40H63N9O8S
- Molecular Weight:830.05
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Barusiban shows affinity for oxytocin receptor (Ki=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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pregnant cynomolgus monkeys injected with oxytocin (OT)[2]
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Dosage:50 or 150 μg/kg
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Administration:Intravenous injection; 50 or 150 μg/kg; once
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 285571-64-4
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Molecular Weight 830.05
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Formula C40H63N9O8S
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Synonyms
FE-200440
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Barusiban Related Classifications
HY-P3516 Related Classifications
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