Navacaprant

产品说明书

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Chemical Structure| 2244614-14-8 同义名 : BTRX-335140;CYM-53093
CAS号 : 2244614-14-8
货号 : A1353911
分子式 : C25H32FN5O2
纯度 : 99%+
分子量 : 453.552
MDL号 : MFCD32215321
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(6.61 mM)，配合低频超声，水浴加热至45℃，并调节pH至4，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Navacaprant (BTRX-335140) is a selective and orally active κ-opioid receptor (KOR) antagonist, exhibiting antagonist activity for κOR, μOR, and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. It possesses favorable in vitro ADMET and in vivo pharmacokinetic profiles, as well as a medication-like duration of action in rats. Navacaprant penetrates well into the CNS and can be utilized for neuropathy research [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL
参考文献

[1]Guerrero M, et al. Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140). J Med Chem. 2019 Feb 28;62(4):1761-1780.