Atosiban acetate
(Synonyms: 醋酸阿托西班; RW22164 acetate; RWJ22164 acetate) 目录号 : GC39849
An oxytocin receptor antagonist
Cas No.:914453-95-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Atosiban is a peptide analog of oxytocin that antagonizes the human oxytocin receptor (Ki = 81 nM).1 It also binds the vasopressin V1a receptor (Ki = 3.5 nM).1 Because of its effects on the oxytocin receptor, atosiban has tocolytic actions in the acute phase of imminent preterm birth.2,3,4
1.Cirillo, R., Tos, E.G., Schwarz, M.K., et al.Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptorJ.Pharmacol. Exp. Ther.306(1)253-261(2003) 2.Lamont, R.F.The development and introduction of anti-oxytocic tocolyticsB. J. O. G.110 (Suppl 20)108-112(2003) 3.Moutquin, J.M., Sherman, D., Cohen, H., et al.Double-blind, randomized, controlled trial of atosiban and ritodrine in the treatment of preterm labor: a multicenter effectiveness and safety studyAm. J. Obstet. Gynecol.182(5)1191-1199(2000) 4.Romero, R., Sibai, B.M., Sanchez-Ramos, L., et al.An oxytocin receptor antagonist (atosiban) in the treatment of preterm labor: A randomized, double-blind, placebo-controlled trial with tocolytic rescueAm. J. Obstet. Gynecol.182(5)1173-1183(2000)
| Cas No. | 914453-95-5 | SDF | |
| 别名 | 醋酸阿托西班; RW22164 acetate; RWJ22164 acetate | ||
| Canonical SMILES | O=C([C@H](CSSCCC(N[C@@H](C1=O)CC2=CC=C(OCC)C=C2)=O)NC([C@@H](NC(C(NC([C@](N1)([H])[C@@H](C)CC)=O)[C@H](O)C)=O)CC(N)=O)=O)N(CCC3)[C@@H]3C(N[C@@H](CCCN)C(NCC(N)=O)=O)=O.OC(C)=O | ||
| 分子式 | C45H71N11O14S2 | 分子量 | 1054.24 |
| 溶解度 | DMSO : 100 mg/mL (94.86 mM; Need ultrasonic); H2O : 50 mg/mL (47.43 mM; Need ultrasonic) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9486 mL | 4.7428 mL | 9.4855 mL |
| 5 mM | 0.1897 mL | 0.9486 mL | 1.8971 mL |
| 10 mM | 0.0949 mL | 0.4743 mL | 0.9486 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Simulated Y-site compatibility of Atosiban acetate with selected intravenous drugs
Eur J Obstet Gynecol Reprod Biol 2022 Aug;275:106-109.PMID:35779331DOI:10.1016/j.ejogrb.2022.06.006.
Objective: The physical compatibility of atosiban and selected drugs during simulated Y-site administration was evaluated. We also searched for any compatibility predictions regarding its physicochemical properties. Study design: Test admixtures were prepared by mixing 5 mL of each study drug solution with 5 mL of atosiban solution in a 1:1 ratio to simulate Y-site infusion. Assessments were made immediately after mixing (baseline), and at 0.5, 1, and 3 h. Visual incompatibility was defined as a presence of haze or any visible particulate matter, gas formation, or colour change. Turbidity and pH variation of the admixtures were also assessed using instrumental methods. Results: None of the admixtures used with atosiban exhibited visual changes and no incompatibility regarding instrumental methods were observed, because no admixture had an increase of 0.5 nephelometric turbidity units, and no pH change was above one unit when compared to baseline. However, the pH of ampicillin and omeprazole admixtures fell outside of the atosiban stability range. Conclusions: Our study showed no physical incompatibility between atosiban and the test drugs in terms of visual changes or nephelometric and pH measurements. However, we recommend against atosiban and ampicillin or omeprazole coadministration until complementary compatibility studies are performed.
A novel HPLC method for analysis of atosiban and its five related substances in Atosiban acetate injection
J Pharm Biomed Anal 2020 Jan 5;177:112808.PMID:31585328DOI:10.1016/j.jpba.2019.112808.
Consulting the national pharmacopoeia, no official quality standard was found for estimation of related substances and assay of Atosiban acetate injection, of which main active component is atosiban. To solve this problem, herein, a novel high performance liquid chromatographic (HPLC) method was developed and validated in this study. A chromatographic system comprising an Inertsil ODS-2 analytical column, mobile phase-A of water (pH adjusted to 3.2 with trifluoroacetic acid)-acetonitrile-methanol (77:14:9, v/v/v), mobile phase-B of acetonitrile-methanol (65:35, v/v), a flow rate of 1.0 mL min-1 and a UV detector set at 220 nm with column temperature at 35 °C has shown simple, reproducible and specific determination for atosiban and its five related substances. Also, we combined with mass spectrometry to characterize the molecular weight and tentative structure of the impurities. Using HPLC verified methodology, results of the validation study showed that the precision, specificity and accuracy of the five impurities, good linear equation R squared was greater than 0.9993, and as such, the limit of detection and the limit of quantification have been determined. The proposed method in this study, which, to the best of our knowledge, is the most comprehensive HPLC determination applied to the routine analysis in quality control of this injection.