生物活性 体外研究 体内研究
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ML-00253764 HYDROCHLORIDE

ML-00253764 HYDROCHLORIDE,1706524-94-8,结构式
ML-00253764 HYDROCHLORIDE
  • CAS号:1706524-94-8
  • 英文名:ML-00253764 (hydrochloride)
  • 中文名:ML-00253764 HYDROCHLORIDE
  • CBNumber:CB84667027
  • 分子式:C18H19BrClFN2O
  • 分子量:413.72
  • MOL File:1706524-94-8.mol
ML-00253764 HYDROCHLORIDE化学性质
  • 储存条件 :Store at -20°C
  • 溶解度 :DMF: 30mg/mL; DMF:PBS (pH 7.2) (1:20): 0.5mg/mL; DMSO: 25mg/mL; Ethanol: 1mg/mL
  • 形态 :A crystalline solid
  • 颜色 :Off-white to light yellow

ML-00253764 HYDROCHLORIDE性质、用途与生产工艺

  • 生物活性 ML-00253764 是一种非肽类黑皮质素受体4 (MC4R) 拮抗剂,其 Ki 和 IC50 值分别为 0.16 µM 和 0.103 µM。脑渗透剂。
  • 体外研究

    ML-00253764 displaces NDP-α-MSH binding with a mean IC 50 of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively. ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes.

  • 体内研究

    ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) shows protection against tumor-induced body weight loss upon chronic, peripheral dosing in CT-26 tumor bearing BALB/c mice.ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 ml/kg.

    Animal Model: CT-26 tumor bearing BALB/c mice
    Dosage: 3, 10, or 30 mg/kg
    Administration: Subcutaneous injection; 3, 10, or 30 mg/kg; once daily
    Result: Reduced tumor-induced weight loss in a mouse model.
ML-00253764 HYDROCHLORIDE上下游产品信息
上游原料
下游产品
ML-00253764 HYDROCHLORIDE生产厂家
  • 公司名称:TOCRIS-US
  • 联系电话:--
  • 电子邮件:customerservice@tocris.co.uk
  • 国家:英国
  • 产品数:5726
  • 优势度:77