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.
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- No. CAS: 285571-64-4
- Fòrmula: C40H63N9O8S
- Peso molecular:830.05
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 285571-64-4
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Peso molecular 830.05
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Fòrmula C40H63N9O8S
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Synonyms
FE-200440
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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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