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当前位置: 首页 > 产品中心 > Small_molecule > Medchemexpress/Macitentan(同义词:ACT-064992)/HY-14184/50mg
商品详细Medchemexpress/Macitentan(同义词:ACT-064992)/HY-14184/50mg
Medchemexpress/Macitentan(同义词:ACT-064992)/HY-14184/50mg
Medchemexpress/Macitentan(同义词:ACT-064992)/HY-14184/50mg
商品编号: HY-14184-10mM*1mLinDMSO
品牌: MedChemExp
市场价: ¥1300.00
美元价: 780.00
产地: 美国(厂家直采)
公司:
产品分类: 小分子
公司分类: Small_molecule
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
Description

Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

In Vitro

Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan, also reducing the expression of mesenchymal markers and restoring CD31 expression and the imbalance between VEGF-A and VEGF-A165b[1]. Macitentan inhibits OATP1B1-mediated uptake of atorvastatin and OATP1B3-mediated uptake of estrone-3-sulfate with IC50 ± SE values of 6.3 ± 0.7 and 11.8 ± 5.0 μM, respectively[3]. Treatment with macitentan or with ACT-132577 does not lead to intracellular accumulation of R123 in HeyA8-MDR, showing that these compounds are not P-gp inhibitors[4].

In Vivo

Macitentan (25 mg/kg/day, p.o.) prevents increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increases extracellular matrix protein production in type 2 diabetes in type 2 diabetes[2]. Macitentan (10 mg/kg, p.o.) coupled with once-per-week 5 mg/kg taxol, significantly reduces the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg, but not 5 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduces the number of proliferating Ki-67-positive cells[4].

Clinical Trial
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References
  • [1]. Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228.

    [2]. Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13.

    [3]. Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78.

    [4]. Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47.

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.6999 mL 8.4995 mL 16.9990 mL
5 mM 0.3400 mL 1.6999 mL 3.3998 mL
10 mM 0.1700 mL 0.8499 mL 1.6999 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[2]

Macitentan is prepared in food admix.

Male db/db mice and age and sex-matched controls (27-32 g) are used for the assay. RandomLy selected diabetic animals are monitored for either 2 months or for 4 months after onset of diabetes. Groups (n=7/group) of the diabetic mice are subjected to oral macitentan treatment for the same period (25 mg/kg/day, food admix). The animals are monitored through assessment of body weight and blood glucose. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • [1]. Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228.

    [2]. Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13.

    [3]. Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78.

    [4]. Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47.

Molecular Weight

588.27

Formula

C₁₉H₂₀Br₂N₆O₄S

CAS No.

441798-33-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity: 99.95%

Data Sheet (118 KB) SDS (120 KB)

COA (92 KB) HNMR (391 KB) LCMS (202 KB)

Handling Instructions (1252 KB)
  • [1]. Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228.

    [2]. Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13.

    [3]. Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78.

    [4]. Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47.

品牌介绍
托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH,5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50~89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者,应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射,并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似,均可达81%~100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用,可加快代谢,故快代谢型者需增加剂量,慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶,熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride):C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应,可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品