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Atosiban/阿托西班 {[allProObj[0].p_purity_real_show]}

货号:A600380 同义名: RW22164; RWJ22164

Atosiban是一种九肽类加压素/催产素受体拮抗剂,可用作宫缩抑制剂,用于自发性早产的研究。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Atosiban/阿托西班 化学结构 CAS号:90779-69-4
Atosiban/阿托西班 化学结构
CAS号:90779-69-4
Atosiban/阿托西班 3D分子结构
CAS号:90779-69-4
Atosiban/阿托西班 化学结构 CAS号:90779-69-4
Atosiban/阿托西班 3D分子结构 CAS号:90779-69-4
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Atosiban/阿托西班 纯度/质量文件 产品仅供科研

货号:A600380 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Vasopressin receptor 1 Vasopressin receptor 2 其他靶点 纯度
Conivaptan HCl 98%
Tolvaptan ++++

vasopressin receptor 2, IC50: 3 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Atosiban/阿托西班 生物活性

描述 Atosiban is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban inhibits the oxytocin-mediated release of IP3 from the myometrial cell membrane. There is reduced release of intracellular, stored calcium from the sacroplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua[3]. Atosiban resulted in fewer maternal side-effects than nifedipine, with no difference in pregnancy prolongation[4].

Atosiban/阿托西班 细胞实验

Cell Line
Concentration Treated Time Description References
Rat small mesenteric artery 0.3 – 3 μM 60 min Atosiban competitively antagonized OT-induced contractions of the rat SMA but caused concentration-dependent steepening of the AVP E/[A] curve (Hill slope increase), indicating receptor heterogeneity. Br J Pharmacol. 1998 Oct;125(4):865-73
Rat aortic rings 0.3 – 10 μM 60 min Atosiban competitively antagonized AVP- and OT-induced contractions of the rat aorta, with Schild slope parameters not significantly different from unity (b=0.82 ± 0.10 and 0.81 ± 0.14) and pKB values of 6.19 ± 0.06 and 6.30 ± 0.04 against AVP and OT, respectively. Br J Pharmacol. 1998 Oct;125(4):865-73
human myometrial strips 1 µM Atosiban antagonized oxytocin (OT)-induced dose-dependent (10-3000 nM) phasic contractions Br J Pharmacol. 2001 Sep;134(1):206-14

Atosiban/阿托西班 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
California mice Unstressed female mice Bilateral NAc core injection 1 ng Single injection, social interaction test conducted 30 minutes later Atosiban infusion in the NAc reduced social approach but did not induce social vigilance in unstressed females. Neuropsychopharmacology. 2020 Aug;45(9):1423-1430
ICR mice Tamoxifen-induced adenomyosis mouse model Intraperitoneal injection 1 mg/kg Once daily for 3 weeks To evaluate the effects of Atosiban on tamoxifen-induced adenomyosis in mice. Results showed that Atosiban significantly prolonged the hotplate response latency, indicating its analgesic effect, but did not significantly reduce the depth of myometrial infiltration. Drug Des Devel Ther. 2025 Apr 2;19:2533-2549
Male Sprague-Dawley rats Single prolonged stress (SPS) model Intraperitoneal injection 5 mg/kg Single administration, followed by behavioral test observations Atosiban blocked the ameliorative effect of oxytocin (OXT) on SPS-induced social behavior deficits, indicating the importance of the OXT signaling pathway in PTSD-related social behavior impairments. J Biomed Sci. 2019 Mar 21;26(1):26

Atosiban/阿托西班 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00599898 Labor, Premature Phase 4 Completed - Israel ... 展开 >> HaEmek Medical Center Afula, Israel, 18100 收起 <<
NCT01796522 Preterm Delivery. Phase 3 Withdrawn(have been published ... 展开 >>new studies that it showed the ineffectiveness of the treatments proposed in this study.) 收起 << May 2013 Spain ... 展开 >> Hospital Universitari y Politécnic La Fe Valencia, Spain, 46026 收起 <<
NCT02292784 Obstetric Labour, Premature Phase 2 Phase 3 Recruiting July 29, 2022 -

Atosiban/阿托西班 参考文献

[1]Sanu O, Lamont RF. Critical appraisal and clinical utility of atosiban in the management of preterm labor. Ther Clin Risk Manag. 2010 Apr 26;6:191-9.

[2]Akerlund M, Carlsson AM, et al. The effect on the human uterus of two newly developed competitive inhibitors of oxytocin and vasopressin. Acta Obstet Gynecol Scand. 1985;64(6):499-504.

[3]Sanu O, Lamont RF. Critical appraisal and clinical utility of atosiban in the management of preterm labor. Ther Clin Risk Manag. 2010 Apr 26;6:191-9

[4]Ali AA, Sayed AK, El Sherif L, Loutfi GO, Ahmed AMM, Mohamed HB, Anwar AT, Taha AS, Yahia RM, Elgebaly A, Abdel-Daim MM. Systematic review and meta-analysis of randomized controlled trials of atosiban versus nifedipine for inhibition of preterm labor. Int J Gynaecol Obstet. 2019 May;145(2):139-148

Atosiban/阿托西班 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.01mL

0.20mL

0.10mL

5.03mL

1.01mL

0.50mL

10.06mL

2.01mL

1.01mL

Atosiban/阿托西班 技术信息

CAS号90779-69-4
分子式C43H67N11O12S2
分子量 994.19
SMILES Code O=C([C@H]1N(C([C@@H](NC([C@H](CC(N)=O)NC([C@H]([C@H](O)C)NC([C@H]([C@@H](C)CC)NC([C@@H](CC2=CC=C(OCC)C=C2)N3)=O)=O)=O)=O)CSSCCC3=O)=O)CCC1)N[C@@H](CCCN)C(NCC(N)=O)=O
MDL No. MFCD00672436
别名 RW22164; RWJ22164; Tractocile; ORF 22164; Antocin; Atosiban Acetate
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 16 mg/mL(16.09 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 15 mg/mL(15.09 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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