Rotigaptide|355151-12-1|(ZP123)-陌孚医药/Medlife

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Rotigaptide (Synonyms: ZP123)

目录号: PL01554 纯度: ≥99%

CAS No. :355151-12-1

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中文名称	Rotigaptide
英文名称	Rotigaptide
英文别名	Rotigaptide;GAP (WYETH);GFA1W6KO7N;Rotigaptide [USAN:INN];GAP 486;GAP 484;ZP123;ZP 123;Rotigaptide (USAN);GTPL9214;Dipeptide 9f [PMID 19175320];DB13067;Ac-d-Tyr-d-Pro-d-Hyp-Gly-d-Ala-Gly-NH2;D05767;Q7370547;N-Acetyl-d-tyrosyl-d-prolyl-(4S)-4-hydroxy-d-prolylglycyl-d-alanylglycinamide;Glycinamide, N-acetyl-D-tyrosyl-D-prolyl-(4S)-4-hydroxy-D-prolylglycyl-D-alanyl-;(2R,4S)-1-[(2R)-1-[(2R)-2-acetamido-3-(4-hydroxyphenyl
Cas No.	355151-12-1
分子式	C₂₈H₃₉N₇O₉
分子量	617.65
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情

Rotigaptide (ZP123) 是连接蛋白 43 (Cx43) 的特异性调节剂。Rotigaptide 可防止 Cx43 介导的间隙连接 (gap junction) 通讯的解偶联，并在急性代谢应激期间使细胞间通讯正常化。Rotigaptide 是一种抗心律失常肽 (AAP)，有潜力用于心律失常–特别是房颤的相关研究。

生物活性

Rotigaptide (ZP123) is a novel and specific modulator of connexin 43 (Cx43). Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress. Rotigaptide is a potent antiarrhythmic peptide (AAP) with improved stability and has the potential for the investigation of cardiac arrhythmias-specifically atrial fibrillation.

性状

Solid

IC50 & Target[1][2]

IC50: connexin 43 (Cx43)

体外研究(In Vitro)

Rotigaptide (100 nM; 24 hours) has a positive effect on cycloheximide-mediated decrease in Cx43 protein levels in cultured neonatal ventricular myocytes.
Rotigaptide (100 nM; 24 hours) dose not affect INS-1 cell apoptosis itself. And it significantly reduces apoptosis in cytokine-exposed cells ~10% at IL-1b concentrations above 15 pg/ml in rat insulin-producing INS-1 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Rotigaptide (intravenous administration; 300 mg/kg; single dose) treatment in mice and rats does not result in toxicity in either species.
In escalating dose studies, Rotigaptide (continuous intravenous infusion; 5-14 days) in rats (100 mg/kg) and dogs (10 mg/kg) are well tolerated and produces no compound-related effects or histological toxicological findings.
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

Powder -20°C 3 years；In solvent -80°C 6 months

ClinicalTrial

参考文献

[1]. Seyed Mojtaba Ghiasi, et al. The connexin 43 regulator Rotigaptide reduces cytokine-induced cell death in human islets
[2]. Stahlhut M, et al. The antiarrhythmic peptide rotigaptide (ZP123) increases connexin 43 protein expression in neonatal rat ventricular cardiomyocytes.Cell Commun Adhes. 2006 Jan-Apr;13(1-2):21-7.
[3]. Kj?lbye AL, et al. P

溶解度数据	In Vitro: DMSO : 200 mg/mL (323.81 mM; Need ultrasonic)配制储备液

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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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