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Nebentan potassium

(Synonyms: YM598)

目录号: PL13980 纯度: ≥99%

Nebentan potassium (YM598) 是一种有效的具有口服活性的非肽类内皮素受体 (ETA receptor) 拮抗剂，通过 Bosentan (HY-A0013) 修饰得到。Nebentan potassium 抑制 [¹²⁵I] 内皮素-1 与人内皮素 ETA 和 ETB 受体结合，Ki 分别为 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相关研究。

CAS No. :342005-82-7

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中文名称	Nebentan potassium
中文别名	Potassium [6-methoxy-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]{ [(E)-2-phenylvinyl]sulfonyl}azanide
英文名称	Nebentan potassium
英文别名	Potassium [6-methoxy-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]{ [(e)-2-phenylvinyl]sulfonyl}azanide;Carbamodithioic acid, (2-(2-(ethylthio)ethoxy)ethyl)-, monopotassium salt;potassium N-[6-methoxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]-2-phenylethenesulfonamidate;LS-50810;N-(Ethoxyethyl)dithiocarbamic acid potassium salt;(2-(2-(Ethylthio)ethoxy)ethyl)carbamodithioic acid monopotassium salt;potassium N-(ethylthioethoxyethyl)dithiocarbamate;Carbamodithioic acid, (2-(2-(ethylthio)ethoxy)ethyl)-, monopotassium salt; potassium N-[6-methoxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyrimidinyl]-2-phenylethenesulfonamidate; LS-50810; N-(Ethoxyethyl)dithiocarbamic acid potassium salt; (2-(2-(Ethylthio)ethoxy)ethyl)carbamodithioic acid monopotassium salt; potassium N-(ethylthioethoxyethyl)dithiocarbamate;;Nebentan potassium
Cas No.	342005-82-7
分子式	C₂₄H₂₀KN₅O₅S
分子量	529.61
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	Nebentan potassium (YM598) 是一种有效的具有口服活性的非肽类内皮素受体 (ETA receptor) 拮抗剂，通过 Bosentan (HY-A0013) 修饰得到。Nebentan potassium 抑制 [¹²⁵I] 内皮素-1 与人内皮素 ETA 和 ETB 受体结合，Ki 分别为 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相关研究。

产品详情

Nebentan potassium (YM598) 是一种有效的具有口服活性的非肽类内皮素受体 (ET_A receptor) 拮抗剂，通过 Bosentan (HY-A0013) 修饰得到。Nebentan potassium 抑制 [¹²⁵I] 内皮素-1 与人内皮素 ET_A 和 ET_B 受体结合，K_i 分别为 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相关研究。

生物活性

Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ET A receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K i of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.

性状

Solid

IC50 & Target[1][2]

ETA 0.679 nM (Ki) ETB 569 nM (K

体外研究(In Vitro)

Nebentan potassium inhibits the specific binding of [I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner, Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively.
In measurement of intracellular Ca concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Nebentan potassium (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy.
Nebentan potassium (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion.
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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71.
[2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:

溶解度数据	In Vitro: DMSO : 125 mg/mL (236.02 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。

Nebentan potassium

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