Atosiban
(Synonyms: 阿托西班; RW22164; RWJ22164) 目录号 : GC12194
Atosiban是一种催产素和加压素受体的混合拮抗剂，通过竞争性阻断子宫平滑肌上的催产素受体，有效抑制宫缩，延长妊娠时间。
Cas No.:90779-69-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Atosiban is a mixed antagonist of oxytocin and vasopressin receptors. It effectively inhibits uterine contractions and prolongs pregnancy by competitively blocking oxytocin receptors on uterine smooth muscle[1, 2]. Atosiban is a synthetic peptide tocolytic agent that can be used to treat premature labor[3].
In vitro, treatment of human myometrial cells with Atosiban (10μM) significantly reduced oxytocin (OT)-induced intracellular p38 kinase activation and COX-2 upregulation[4]. Treatment of human umbilical vein endothelial cells (HUVECs) with Atosiban (10μM) significantly inhibited the promoter activity of hypoxia-inducible factor-1 α (HIF-1α) in HUVECs and reduced the mRNA and protein expression of HIF-1α[5].
In vivo, treatment of experimental endometriosis rats with Atosiban (0.5mg/kg/day) by intraperitoneal injection for 21 days significantly reduced the volume of endometriotic implants and significantly reduced the expression level of proliferating cell nuclear antigen in implanted tissues[6]. Treatment of pregnant rats with Atosiban (6mg/kg/day) by intraperitoneal injection for 21 days significantly increased the level of oxidative stress in the plasma and heart tissue of newborn rats[7].
References:
[1] McCafferty G P, Pullen M A, Wu C, et al. Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat[J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2007, 293(1): R299-R305.
[2] Kuć P, Laudański P, Pierzyński P, et al. The effect of combined tocolysis on in vitro uterine contractility in preterm labour[J]. Advances in medical sciences, 2011, 56(1): 88-94.
[3] Di Renzo G C. Safety and efficacy of new drugs in preterm labor[J]. Expert Review of Obstetrics & Gynecology, 2007, 2(1): 19-24.
[4] Kim S H, Pohl O, Chollet A, et al. Differential effects of oxytocin receptor antagonists, Atosiban and Nolasiban, on oxytocin receptor–mediated signaling in human amnion and myometrium[J]. Molecular Pharmacology, 2017, 91(4): 403-415.
[5] Zhu J, Wang H, Zhang X, et al. Regulation of angiogenic behaviors by oxytocin receptor through Gli1-indcued transcription of HIF-1α in human umbilical vein endothelial cells[J]. Biomedicine & Pharmacotherapy, 2017, 90: 928-934.
[6] Simsek Y, Celik O, Karaer A, et al. Therapeutic efficiency of Atosiban, an oxytocin receptor blocking agent in the treatment of experimental endometriosis[J]. Archives of gynecology and obstetrics, 2012, 286(3): 777-783.
[7] Simsek Y, Celik O, Karaer A, et al. Elevated cardiac oxidative stress in newborn rats from mothers treated with atosiban[J]. Archives of gynecology and obstetrics, 2012, 285(3): 655-661.
Atosiban是一种催产素和加压素受体的混合拮抗剂，通过竞争性阻断子宫平滑肌上的催产素受体，有效抑制宫缩，延长妊娠时间[1, 2]。Atosiban是一种合成的肽类宫缩抑制剂，能够用于治疗早产[3]。
在体外，Atosiban（10μM）处理人子宫肌层细胞，显著降低了催产素（OT）诱导的细胞内p38激酶活化和COX-2的上调[4]。Atosiban（10μM）处理人脐静脉内皮细胞（HUVECs），显著抑制了HUVECs中缺氧诱导因子-1 α（HIF-1α）的启动子活性，降低了HIF-1α的mRNA和蛋白表达[5]。
在体内，Atosiban（0.5mg/kg/day）通过腹腔注射治疗实验性子宫内膜异位症大鼠21天，显著减小了子宫内膜异位症植入物的体积，显著降低了植入组织的增殖细胞核抗原表达水平[6]。Atosiban（6mg/kg/day）通过腹腔注射处理妊娠大鼠21天，显著升高了新生鼠仔血浆和心脏组织的氧化应激水平[7]。
| Cell experiment [1]: | |
Cell lines | Prenatal myometrial smooth muscle cells |
Preparation Method | Prenatal myometrial smooth muscle cells were stimulated with oxytocin (OT) (10nM) in the presence or absence of Atosiban (10μM) for 5min, 15min, 30min, 2h, 4h, and 6h. The expression of phosphorylated NF-κB p65 subunit, ERK1/2, and p38 MAPK, as well as COX-2 and p-cPLA2 were detected by Western blotting. |
Reaction Conditions | 10μM; 5min, 15min, 30min, 2h, 4h, and 6h |
Applications | Treatment with Atosiban significantly reduced the OT-driven activation of p38 kinase and the upregulation of COX-2 in human myometrial cells. |
| Animal experiment [2]: | |
Animal models | Female Wistar rats |
Preparation Method | Endometriosis was surgically induced in 35 female rats during estrus. Four weeks after this procedure, relaparotomy was performed. The viability and dimensions of the endometriosis foci were recorded. Rats were then randomly divided into three groups. In the first group (n=8), a daily dose of 0.2mL 0.9% NaCl was injected intraperitoneally (i.p.) (control cases). In the second and third groups (n=8 and n=8), 0.5mg/kg/day i.p. Atosiban and 1mg/day i.p. diltiazem were given, respectively. The treatment was continued for 21 consecutive days at approximately the same time each day. At the end of the treatment, laparotomy was performed, and the dimensions of the endometriosis foci were recorded. The endometrial implants were processed for histological and immunohistochemical studies. The volumes of endometriotic implants were measured, and immunohistochemical analyses were performed, and compared between the groups. |
Dosage form | 0.5mg/kg/day; 21 days; i.p. |
Applications | After the treatment with Atosiban, volumes of endometriotic implants decreased significantly. Proliferating cell nuclear antigen expression levels were significantly reduced in the Atosiban and diltiazem groups compared with the control group. |
References: | |
| Cas No. | 90779-69-4 | SDF | |
| 别名 | 阿托西班; RW22164; RWJ22164 | ||
| 分子式 | C43H67N11O12S2 | 分子量 | 994.19 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 14 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at -20°C |
| 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。 |
||
| 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 | 1.0058 mL | 5.0292 mL | 10.0584 mL |
| 5 mM | 0.2012 mL | 1.0058 mL | 2.0117 mL |
| 10 mM | 0.1006 mL | 0.5029 mL | 1.0058 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet