Carbetocin acetate|1631754-28-3|(卡贝缩宫素醋酸盐)-陌孚医药/Medlife

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Carbetocin acetate (Synonyms: 卡贝缩宫素醋酸盐)

目录号: PL08657 纯度: ≥99%

CAS No. :1631754-28-3

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中文名称	Carbetocin acetate
英文名称	Carbetocin acetate
英文别名	Carbetocin (acetate);Carbetocin acetate;D81076
Cas No.	1631754-28-3
分子式	C₄₇H₇₃N₁₁O₁₄S
分子量	1048.21
包装储存	Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

产品详情

Carbetocin acetate 是一种催产素 (OT) 类似物，是催产素受体 (oxytocin receptor) 激动剂，K_i 是 7.1 nM。Carbetocin acetate 对催产素受体的嵌合 N 末端 (E1) 具有高亲和力 (K_i=1.17 μM)。Carbetocin acetate 具有用于产后出血研究的潜力。Carbetocin acetate 能透过血脑屏障，可以通过激活 CNS 中的催产素受体而具有类抗抑郁活性。

生物活性

Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a K i of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (K i =1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.

性状

Solid

体外研究(In Vitro)

Carbetocin acetate is an agonist with about 10-fold lower affinity for the oxytocin receptor but with significantly higher stability and a longer duration of action. Carbetocin acetate has higher affinity to the chimeric E1 receptor and especially to each of the combinations of E1 with the other extracellular domains, i.e. chimeric receptors E13 (Ki=13 nM), E123 (Ki=56 nM), and E1234 (Ki=37 nM).
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Carbetocin (2-20 mg/kg; i.p.) acetate has a significant effect of treatment on the percent time spent climbing, swimming and immobile.
Carbetocin (1, 10,100 μg/rat, i.c.v.) acetate reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

ClinicalTrial

参考文献

[1]. Stella Chaviaras, et al. Assessing the antidepressant-like effects of carbetocin, an oxytocin agonist, using a modification of the forced swimming test. Psychopharmacology (Berl). 2010 May;210(1):35-43.
[2]. Gerald Gimpl, 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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (119.25 mM; ultrasonic and warming and heat to 60°C)H₂O : 10 mg/mL (9.54 mM; ultrasonic and warming and heat to 60°C)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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