LY2955303

产品说明书

Print
Chemical Structure| 1433497-19-8 同义名 : -
CAS号 : 1433497-19-8
货号 : A119600
分子式 : C36H42N4O3
纯度 : 99%
分子量 : 578.74
MDL号 : MFCD31561443
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 LY2955303 is a potent and selective RARγ antagonist with IC50 of 1.1nM without effect on RARα and RARβ. LY2955303 shows good pharmacokinetic properties with less unacceptable adverse effects on testes compared with pan-RAR antagonist like BMS-189453. A single oral dose of LY2955303 demonstrated a dose responsive effect whereby the mono-iodoacetate rat model, with OA-like joint pain, reduced differential weight bearing (ED50 = 0.72 mg/kg). The toxicity of LY2955303 for testicular degeneration will not be observed until the dose up to 30mg/kg.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.64mL

1.73mL

0.86mL

17.28mL

3.46mL

1.73mL

参考文献

[1]Hughes NE, Bleisch TJ, et al. Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-7.