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Carbetocin (Synonyms: 卡贝缩宫素)
目录号: PC15098 纯度: ≥98%
CAS No. :37025-55-1
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中文名称
Carbetocin
中文别名
卡贝缩宫素;卡比托辛;醋酸卡贝缩宫素;4-异丁基环己烷羧酸 (CIS-, TRANS-混合物);醋酸卡贝缩宫素,卡比托辛;卡贝缩宫素(Carbetocin)
英文名称
Carbetocin
英文别名
Carbetocin;BUTYRYL-TYR(ME)-ILE-GLN-ASN-CYS-PRO-LEU-GLY-NH2, (SULFIDE BOND BETWEEN BUTYRYL-4-YL AND CYS);(BUTYRYL1,TYR(ME)2)-1-CARBAOXYTOCIN TRIFLUOROACETATE SALT;Carbetocin Acetate;Carbansin;CARBETOCIN TRIFLUOROACETATE SALT;DeaMino-2-O-Methyltyrosine-1-carbaoxytocin;Depotocin;M.W. 988.17 C45H69N11O12S
Cas No.
37025-55-1
分子式
C45H69N11O12S.C2Ho2F3
分子量
1102.18
包装储存

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

生物活性

Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin 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 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 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).

Medlife 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.) has a significant effect of treatment on the percent time spent climbing, swimming and immobile.
Carbetocin (1, 10,100 μg/rat, i.c.v.) reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats weighing between 300 and 500 g
Dosage: 2, 6.4, 20 mg/kg
Administration: IP; single dose
Result: Increased climbing with 6.4 mg/kg and resulted in a significantly greater proportion of time spent swimming with 20 mg/kg.
运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

H2O : ≥ 33.33 mg/mL (33.73 mM)

DMSO : ≥ 31 mg/mL (31.37 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0120 mL 5.0599 mL 10.1198 mL
5 mM 0.2024 mL 1.0120 mL 2.0240 mL
10 mM 0.1012 mL 0.5060 mL 1.0120 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.53 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

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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