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Macitentan (Synonyms: 马西替坦; ACT-064992) 纯度: 99.80%
Macitentan (ACT-064992) 是有口服活性,非多肽 ETA 和 ETB (内皮素受体)双拮抗剂。Macitentan 有用于特发性肺纤维化和肺动脉高压的潜力。
Macitentan Chemical Structure
CAS No. : 441798-33-0
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥712 | In-stock | |
5 mg | ¥550 | In-stock | |
10 mg | ¥770 | In-stock | |
50 mg | ¥1400 | In-stock | |
100 mg | ¥1900 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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生物活性 |
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1]. |
IC50 & Target |
ETA/ETB[1] |
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体外研究 (In Vitro) |
Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan (ACT-064992), 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Macitentan (ACT-064992; 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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
588.27 |
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Formula |
C19H20Br2N6O4S |
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CAS 号 |
441798-33-0 |
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中文名称 |
马西替坦 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 50 mg/mL (84.99 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [2] |
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. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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