- Atrasentan hydrochloride
- Avosentan
- Zibotentan (ZD4054)
MacitentanEndothelin (ET)(A) and ET(B) receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.20%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Cell experiment [1,2]: | |
Cell lines | Primary human pulmonary smooth muscle cells, microvascular endothelial cells |
Preparation method | The solubility of this compound in DMSO is >21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | IC50: 1 nM |
Applications | Macitentan completely inhibited intracellular calcium increase induced by ET-1 on primary human pulmonary smooth muscle cells with approximate IC50 of 1 nM. Macitentan inhibited ET-1-induced contractions on isolated rat aortic rings or S6c-induced contractions on isolated rat tracheal rings with pA2 of 7.6 and 5.9, respectively. In microvascular endothelial cells, pretreatment with macitentan restored tube formation ability and reduced the expression of mesenchymal markers and restored CD31 expression and the imbalance between VEGF-A and VEGF-A165b. |
Animal experiment [1,3-5]: | |
Animal models | Hypertensive DOCA-salt rats, monocrotaline rat model of pulmonary hypertension, SKOV3ip1 ovarian cancer model |
Dosage form | Oral administration, 25 mg/kg/day |
Application | In normotensive rats, macitentan increased plasma ET-1 concentration. Macitentan dose-dependently decreased mean arterial blood pressure in hypertensive DOCA-salt rats with a maximal effect of -26 mm Hg at a dose of 10 mg/kg. Oral administration of macitentan dose-dependently prevented the development of pulmonary hypertension and the development of right ventricle hypertrophy with a maximal efficacy of 30 mg/kg/day in monocrotaline rat model of pulmonary hypertension. Chronic oral administration of macitentan at 30 mg/kg/day significantly improved the 42-day survival in monocrotaline rats. Macitentan (25 mg/kg/day, p.o.) prevented increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increased extracellular matrix protein production in type 2 diabetes. Macitentan (10 mg/kg, p.o.) in combination with once-per-week 5 mg/kg taxol significantly reduced the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduced the number of proliferating Ki-67-positive cells. Macitentan (100 mg/kg) treatment combined with paclitaxel (5 mg/kg) reduced tumor incidence and further reduced tumor weight and incidences of ascites in SKOV3ip1 ovarian cancer model. Macitentan plus paclitaxel inhibited the phosphorylation of ETRs and suppressed the survival pathways of tumor cells by decreasing the levels of pVEGFR2, pAkt, and pMAPK. Macitentan enhanced effects of paclitaxel on tumor cells dividing and apoptosis. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Marc Iglarz, Christoph Binkert, Keith Morrison, et al. Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist. Journal of Pharmacology and Experimental Therapeutics, 2008, 327:736-745. [2]. 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. [3]. 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. [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. [5].Kim S J, Kim J S, Kim S W, et al. Macitentan (ACT-064992), a tissue-targeting endothelin receptor antagonist, enhances therapeutic efficacy of paclitaxel by modulating survival pathways in orthotopic models of metastatic human ovarian cancer[J]. Neoplasia, 2011, 13(2): 167-IN12. |
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Cas No. | 441798-33-0 | SDF | Download SDF |
Synonyms | N/A | ||
Chemical Name | 5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine | ||
Canonical SMILES | CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br | ||
Formula | C19H20Br2N6O4S | M.Wt | 588.27 |
Solubility | ≥24.4mg/mL in DMSO | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Macitentan is a new dual ETA/ETB endothelin (ET) receptor antagonist, with mean IC50 values of 0.5 ± 0.2 nM (n= 17) to inhibit the binding of 125I-ET-1 to recombinant ETA receptors, and of 391±182 nM (n= 17) for ETB receptors in Chinese hamster ovary cells [1].
ETA and ETB are ET receptors, both of them mediate the detrimental actions of ET-1, and dual blockade of them may be necessary [1].
In microsomal membranes of human-ETA and ETB-overexpressing Chinese hamster ovary cells, macitentan inhibited the binding between 125I-ET-1 and recombinant ETA receptors, with a mean IC50 value of 0.5 ± 0.2 nM (n= 17). The mean IC50 value for ETB receptors was 391±182 nM (n= 17). Macitentan completely inhibited the effect that ET-1 increased intracellular calcium in non-recombinant cells [1].
Intravenous administrated macitentan had a volume of distribution largely exceeding plasma volume and a terminal half-life of 2 h in rats. Macitentan was hence metabolized to its major and the only circulating metabolite, a dual ET receptor antagonist, ACT-132577. ACT-132577 also had a volume of distribution greater than the plasma volume. It showed a longer half-life than macitentan in rats. In rat, multiple oral dosing of macitentan at a dose of 10 mg/kg led to 4 to 5-fold higher exposure levels of ACT-132577 than those of the parent compound [1].
Reference: [1]. Marc Iglarz, Christoph Binkert, Keith Morrison, et al. Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist. Journal of Pharmacology and Experimental Therapeutics, 2008, 327:736-745.
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医用细胞涂片离心机
医用细胞离心涂片机
医用细胞离心涂片机是第一款使用精密控制的离心技术对细胞进行分离,形成薄层同时还能保持细胞完整的设备。它采用离心原理,将细胞
转移到诊断载玻片的固定区域,样品残液则被过滤卡吸收。通过离心力的作用,细胞结构趋向扁平,故细胞核表达尤为清晰。各种细胞在离
心过程中机会均等,不存在某些细胞或成份被人为过滤的情况,故最能反映细胞的真实环境状态。医用细胞离心涂片机特殊的倾斜结构设计还可避免细
胞在制备过程中丢失
医用细胞离心涂片机的主要特点
●医用细胞离心涂片适用于所有液基样本,尤其是细胞含量低的液基样本,如脑脊液、尿液
●医用细胞离心涂片同时处理12份样本
●医用细胞离心涂片优化的盖门开关,方便人员单手操作
●医用细胞离心涂片医用细胞离心涂片带自锁功能的塑料外盖,且仅有在盖门上锁的情况下,仪器方能进入运行状态
●医用细胞离心涂片标配一个密封舱,可高温高压消毒
●医用细胞离心涂片3级加速控制,保护脆性样品
●符合ICE61010的离心安全标准
●样本安全警报:结束后每分钟报警一次,提醒客户及时取出样本,防止风干
●可选择一次性使用耗材或反复多次使用耗材
医用细胞离心涂片适用于医院临床检验、生物、化学实验室和血站、血浆站对血液等样品的分离,是最新一代具有专门功能的产品。由微机控制,变频电机驱动,无碳刷粉尘污染,内腔由优质不锈钢制成,快速升降,操作简便,噪声低,振动小。
该系列离心机广泛适用于免疫血液学实验室、检验室、研究室,可进行红细胞血清学实验,做抗原、抗体的鉴定及库姆式实验的结果判断等,是各类医院血库,实验室,血站,医学院校和医学研究机构的必备设备。
医用细胞涂片离心机http://www.fameinstrument.cn/
普通生化检查分离血清,这个是用低速离心机转速在3000—3500转。一般在3分钟之内就可以了,分析分离效果,可以酌情调节转速和时间,用试验型的那种小的就行
至于管式离心机分离血清生产疫苗,这个有着严格的工艺规范,只能照做,不能随意更改参数
富一阳光与你交流离心机分离机设备相关问题,希望对你有帮助~
RCF = 1.119 x 10-5 x (rpm)2 x r
其中r 表示离心机转轴中心与离心管中心的距离,单位为cm。由于离心管的位置由转子(rotor)决定,因此r 必须由查阅相关转子的参数而得。
GB 19815-2005 离心机安全要求
GB 6065-1985 TZ立式振动离心机
GB 12258-1990 医用低速离心机
JB/T 3263-2000 卧式振动离心机
JB/T 4064-2005 上悬式离心机
JB/T 5519-1991高速冷冻离心机
JB/T 6118-1992 TCL沉降过滤离心机
JB/T 53190-1999 三足式离心机 产品质量分等
JB 447-1985卧式活塞推料离心机技术条件
JB/T 502-2004 螺旋卸料沉降离心机
JB/T 5284-1991 防爆型刮刀卸料离心机 序号 标 准 代 号 标 准 名 称 1 GB/T 4774-2004 分离机械 名词术语 2 GB 7779-2005 离心机型号编制方法 3 GB 10901-2005 离心机 性能测试方法 4 GB/19815-2005 离心机 安全要求 5 GB/T10894-2004 分离机械 噪音测试方法 6 GB/T10895-2004 离心机 分离机 机械振动测试方法 7 JB/T 447-2004 活塞推料离心机 8 JB/T 10411-2004 离心机、分离机奥氏体钢锻件超声检测及质量评级 9 JB/T 8051-2006 离心机转鼓强度计算规范 10 JB/T 8865-2001 活塞推料离心机用滤网 11 JB/T 9095-1999 离心机、分离机锻焊件无损探伤技术规范 12 JB/T 7217-2006 分离机械涂装通用技术条件 13 JB/T 6418-2006 分离机械 清洁度测定方法向左转|向右转
1.冷凝器积垢:冷凝器换热管内表水质积垢(开式循环的冷却水系统最容易积垢),而导致传热热阻增大,换热效果降低,使冷凝温度升高或蒸发温度降低,另外,由于水质未经处理和维护不善,同样造成换热管内表面沉积沙土、杂质、藻类等物,造成冷凝压力升高而导致离心机喘振发生。
2.制冷系统有空气:当离心机组运行时,由于蒸发器和低压管路都处于真空状态,所以连接处极容易渗入空气,另外空气属不凝性气体,绝热指数很高,为1.4,当空气凝积在冷凝器上部时,造成冷凝压力和冷凝温度升高,而导致离心机喘振发生。
3.冷却塔冷却水循环量不足,进水温度过高等。由于冷却塔冷却效果不佳而造成冷凝压力过高,而导致喘振发生。
4.蒸发器蒸发温度过低:由于系统制冷剂不足、制冷量负荷减小,球阀开启度过小,造成蒸发压力过低而喘振。
5.关机时未关小导叶角度和降低离心机排气口压力。当离心机停机时,由于增压突然消失,蜗壳及冷凝器中的高压制冷剂蒸气倒灌,容易喘振。
离心机喘振排除
1.冷凝器结垢:清除传热面的污垢和清洗冷却塔。
2.系统中空气排除:离心机采用K11制冷剂时,一般液体温度超过28℃ 时,表明系统中有空气存在。排除方法:启动抽气回收装置,将不凝性气体排出,一般将制冷剂R11的压力抽到稍低于制冷荆液体温度相对应的饱和压力,即28℃以下的对应压力:117.68KMP以下即可。
3.启动后发生喘振:进行反喘振调节。当能量调节大幅度减少时,造成吸气量不足,即蒸气不能均匀流入叶轮,导致排气压力陡然下降,压缩机处于不稳定工作区,而发生喘振。为了防止喘振,可将一部分被压缩后的蒸气,由排气管旁通到蒸发器,不但可防喘振.而且对离心机启动时也有益:减少蒸气密度和启动时的压力,可减小启动功率。
4.蒸发压力过低:检查蒸发压力过低原因,制冷剂不足添加制冷剂,制冷量负荷小,关闭能量调节叶片。
5.停机时喘振:停离心机时应注意主电机有无反转现象,并尽可能关小导叶角度,降低离心机排气口压力。
离心机操作过程中,应保持冷凝压力和蒸发压力的稳定,使离心机制冷量高于喘振点对应制冷量,以防喘振