Arotinolol|68377-92-4|(阿罗洛尔)-陌孚医药/Medlife

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Arotinolol (Synonyms: 阿罗洛尔)

目录号: PL14312 纯度: ≥98%

CAS No. :68377-92-4

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中文名称	Arotinolol
中文别名	阿罗洛尔;5-[2-3-叔丁基氨基-2-羟基丙基硫]-4-噻唑基]-2-噻吩甲酰氨;阿罗洛尔碱;克拉利宾
英文名称	Arotinolol
英文别名	5-(2-((3-(tert-Butylamino)-2-hydroxypropyl)thio)thiazol-4-yl)thiophene-2-carboxamide;2-(3-tert-butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-thien-2-yl)-thiazole;2-Thiophenecarboxamide,5-[2-[[3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazolyl]-;5-(2-(3-(TERT-BUTYLAMINO)-2-HYDROXYPROPYLTHIO)THIAZOL-4-YL)THIOPHENE-2-CARBOXAMIDE;5-[2-[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl-1,3-thiazol-4-yl]thiophene-2-carboxamide;Arotinolol;(+/-)- [2-[[3-[(1,1-dimethylethyl)-amino]-2-hydroxypropyl]thio]-4-thiazolyl]-2-thiophenecarboxamide;2-(3-tert-butylamino-2-hydroxypropylthio);2-(3-tert-Butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-2-thienyl)thiazole;2-Thiophenecarboxamide, 5-[2-[[3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazolyl]-, (+-)-;5-[2-[3-(tert-butylamino)-2-hydroxy-propyl]sulfanyl-1,3-thiazol-4-yl]thiophene-2-carboxamide;Arotinolo;Arottnolol
Cas No.	68377-92-4
分子式	C₁₅H₂₁N₃O₂S₃
分子量	371.54
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Arotinolol 是一种非选择性的 α/β-肾上腺素受体 (α/β-adrenergic receptor ) 阻滞剂和一种血管扩张性 β-受体阻滞剂。Arotinolol 也显示出抑制放射性配体 ¹²⁵I-ICYP 与 5HT_1B-羟色胺受体能结合的能力。Arotinolol 是一种抗高血压试剂，可用于研究各种心血管疾病。

生物活性

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand I-ICYP to 5HT 1B -serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.

性状

Solid

IC50 & Target[1][2]

5-HT2A Receptor

体外研究(In Vitro)

Arotinolol shows its selectivity of β-adrenergic receptors, the result of Arotinolol for β1 and β2 adrenoceptors in I-ICYP binding to rat cerebral cortical membranes with pKi value of 9.74 and 9.26 respectively. The selectively of β1 and β2 is equal.
Arotinolol shows its potency for inhibiting the binding of the same radioligand to 5HT1B-serotonergic receptor site, Arotinolol displaces I-ICYP binding to 5HT1B-receptors with the pKi values of 7.97 and 8.16 resepectively for β1 and β2 adrenergic receptors.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Arotinolol (oral gavage; 200 mg/kg; 8 weeks) can significantly decrease central arterial pressure (CAP) and pulse wave velocity (PWV), in addition, it reduces aortic collagen depositions and finally improves arterial stiffness in SHR mouse.
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；4°C 2 years

ClinicalTrial

参考文献

[1]. Zhou W, et al. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats.PLoS One. 2014 Feb 12;9(2):e88722.
[2]. Hiroshi TSUCHIHASHI, et al. Characteristics of 1251-lodocyanopindolol Binding to 8-Adrenergic and Serotonin-1B Receptors of Rat Brain: Selectivity of 19-Adrenergic Agents

溶解度数据	In Vitro: DMSO : 125 mg/mL (336.44 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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