| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M409076-1ml |
1ml |
现货  |
|
| 别名 | 马西腾坦 (ACT 064992) |
|---|---|
| 英文别名 | Sulfamide, N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Macitentan (ACT 064992) |
| 生化机理 | 马西替坦（ACT 064992）是一种口服活性非肽类 ETA/ETB（内皮素）双重受体拮抗剂，IC50 为 0.5 nM/391 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 拮抗剂 |
| 作用机制 | 内皮素受体，ET-A/ET-B 拮抗剂 |
| 产品介绍 |
Macitentan是一种口服有效的，非肽类，ETA/ETB(内皮素) receptor双重拮抗剂，IC50为0.5 nM/391 nM。 Information Macitentan (ACT 064992) Macitentan (ACT 064992) is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM. Macitentan achieves full inhibition of intracellular calcium increase induced by ET-1 on primary human pulmonary smooth muscle cells with approximate IC50 of 1 nM. Macitentan inhibits 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 vivo Macitentan administered to normotensive rats, increases plasma ET-1 concentration, which occurred at a 10-fold lower dose than with bosentan. Macitentan dose-dependently decreases mean arterial blood pressure in hypertensive DOCA-salt rats with a maximal effect of -26 mm Hg at a dose of 10 mg/kg and a ED50 of 1mg/kg. At the maximal effective dose, the duration of the blood pressure response to Macitentan is approximately 40 hr. Macitentan orally administrated dose-dependently preventes 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 improves the 42-day survival in monocrotaline rats (83 vs 50% survival in macitentan vs vehicle; 66% reduction of mortality at 42 days). Macitentan (30 mg/kg/day) treated for 24 h partially prevents the development of renal vasoconstriction and increases renal blood flow in streptozotocin-induced diabetic rat model. Macitentan increases glomerular filtration rate and decreases filtration fraction, and attenuates vascular and tubulo-interstitial lesions and also glomerular damage. Macitentan (25 mg/kg/day, p.o.) attenuates the increase of renal, cardiac and retinal ET-1, TGF-β1, VEGF, FN, EDB+FN, collagenα-I(IV) mRNA expression along with increased FN, collagen protein and NF-κB activation induced by type 2 diabetes in db/db mice. Macitentan also ameliorates mesangial expansion, cardiac dysfunction and the increased expression of ANP and BNP in these diabetic mice. Macitentan (100mg/kg) treatment combined with paclitaxel (5 mg/kg) reduced tumor incidence (5/9 vs 9/9 of paclitaxel along) and further reduces tumor weight (median [range]: 0.1 vs 0.4 g of paclitaxel along) and incidences of ascites (0/9 vs 4/9 of paclitaxel along) in SKOV3ip1 ovarian cancer model when compared with paclitaxel alone. Macitentan plus paclitaxel inhibits the phosphorylation of ETRs and suppresses the survival pathways of tumor cells by decreasing the levels of pVEGFR2, pAkt, and pMAPK. Macitentan enhances effects of paclitaxel on tumor cells dividing (Brud+ cells: 18.5 vs 30.8 of paclitaxel along) and apoptosis (TUNEL+ cells: 195 vs 150 of paclitaxel along). cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| ALogP | 3.671 |
|---|---|
| hba_count | 8 |
| HBD Count | 2 |
| Rotatable Bond | 11 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCCN[S](=O)(=O)NC1=NC=NC(=C1C2=CC=C(Br)C=C2)OCCOC3=NC=C(Br)C=N3 |
| 分子量 | 588.27 |
| Reaxy-Rn | 11340634 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11340634&ln= |
| DMSO(mg / mL) Max Solubility | 100 |
|---|---|
| DMSO(mM) Max Solubility | 169.99 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 11340634 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11340634&ln= |
| Concentration(Compounding value) | 9-11（mmol/L） |
|---|---|
| Record the entire process by video | Conform |
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