• 咨询热线
    客服服务热线 13671568941/15317326293
  • 在线咨询
  • 微信客服
    微信客服
  • 公众号
    扫码关注公众号

Fulacimstat

CAS No. 1488354-15-9

Fulacimstat ( BAY 1142524 | BAY1142524 | BAY-1142524 )

产品货号. M12057 CAS No. 1488354-15-9

Fulacimstat (BAY 1142524, BAY1142524) 是一种有效的口服食糜酶抑制剂,对人和仓鼠食糜酶的 IC50 分别为 4 nM 和 3 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥2341 有现货
10MG ¥3345 有现货
25MG ¥5605 有现货
50MG ¥7979 有现货
100MG ¥10773 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Fulacimstat
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    Fulacimstat (BAY 1142524, BAY1142524) 是一种有效的口服食糜酶抑制剂,对人和仓鼠食糜酶的 IC50 分别为 4 nM 和 3 nM。
  • 产品描述
    Fulacimstat (BAY 1142524, BAY1142524) is a potent, orally available chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively; blocks the generation of profibrotic chymase-dependent factors such as Ang II, ET-1, and TGF-β1 in vitro with a nanomolar IC50; reduces isoprenaline-induced cardiac fibrosis and attenuates the deterioration of heart function after MI, increases left-ventricular ejection fraction in dogs with LVD induced by intracoronary microembolization with no effects on blood pressure or heart rate.?Other Indication Phase 2 Clinical(In Vitro):Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.(In Vivo):Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation.
  • 体外实验
    Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively.
  • 体内实验
    Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation.
  • 同义词
    BAY 1142524 | BAY1142524 | BAY-1142524
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Other Targets
  • 研究领域
    Other Indications
  • 适应症
    Other Disease

化学信息

  • CAS Number
    1488354-15-9
  • 分子量
    487.39
  • 分子式
    C23H16F3N3O6
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : 5 mg/mL 10.26 mM
  • SMILES
    O=C(C1=CN(C2=CC=C3N(C)C(OC3=C2)=O)C(N([C@@H]4CCC5=C4C=CC=C5C(F)(F)F)C1=O)=O)O
  • 化学全称
    1-(3-methyl-2-oxo-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]pyrimidine-5-carboxylic acid

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1.?Kanefendt F, et al. Clin Pharmacol Drug Dev. 2018 Jun 7. doi: 10.1002/cpdd.579. 2.?Hanna Tinel, et al. Abstract 13624: A Novel Chymase Inhibitor BAY 1142524 Reduces Fibrosis and Improves Cardiac Function After Myocardial Infarction in Hamster. Circulation. 2017;136:A13624.
产品手册
关联产品
  • Sitafloxacin Hydrate

    西他沙星(INN;也称为 DU-6859a)是一种氟喹诺酮类抗生素,在治疗布鲁里溃疡方面显示出良好的前景。

  • 3',4',5',5,7-Pentame...

    3',4',5',5,7-Pentamethoxyflavanone 是一种天然黄酮化合物,在 Neoraptua magnifica var. magnifica 中发现。

  • Orexin A (human, rat...

    Endogenous agonist at orexin receptors (Ki values are 20 and 38 nM for OX1 and OX2 receptors respectively). Stimulates feeding following central administration and may be involved in the control of sleep-wake cycle and other hypothalamic functions.