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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 285571-64-4
- 分子式: C40H63N9O8S
- 分子量:830.05
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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 |
化学情報
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CAS 番号 285571-64-4
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分子量 830.05
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分子式 C40H63N9O8S
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別名
FE-200440
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Barusiban 関連分類
HY-P3516 関連分類
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