BTRX-335140 (CYM-53093) 是一种有效且选择性的口服 κ opioid receptor (KOR) 拮抗剂，对 κOR，μOR 和 δOR 具有拮抗剂活性，IC50 值分别为 0.8 nM，110 nM 和 6500 nM。BTRX-335140 在大鼠中具有良好的体外 ADMET 和体内药代动力学特征。BTRX-335140 可以很好地分布到 CNS 中。 ADMET (吸收，分布，代谢，排泄和毒性)。
货号:ajcx16470
CAS:2244614-14-8
分子式:C25H32FN5O2
分子量：453.55
溶解度:DMSO: 16.67 mg/mL (36.75 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) [1].

[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.