BTRX-335140

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

BTRX-335140 是一种有效、选择性、口服活性 κ 阿片受体 (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 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 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) . BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.

Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor. Cell Viability Assay Cell Line:OPRK1-BLA U2OS cells Concentration:0-10 μM Incubation Time:4 hours Result:Exibited antagonist activity to KOR, DOR and MOR with IC50 values of 0.8, 110 and 6500 nM respectively, and showed selective antagonist activity to KOR.

Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment.Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water.Animal Model:Rat PRL model Dosage:0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg Administration:Oral gavage; 0.01-3 mg/kg onceResult:Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.Animal Model:Adult male ICR mice with tail dipped into 50°C hot water Dosage:1 mg/kg Administration:Intraperitoneal injection; 1 mg/kg once Result:Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.

CYM-53093

Endocrinology/Hormones

Opioid Receptor

δ-opioid receptor|κ-opioid receptor|μ-opioid receptor

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2244614-14-8

453.55

C25H32FN5O2

>98% (HPLC)

DMSO:16.67 mg/mL (36.75 mM; Need ultrasonic)

CCc1cc2c(C)c(-c3nc(C)no3)c(N(CC3)CCC3NC3CCOCC3)nc2c(F)c1

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(-20℃)

With Ice Pack

≥ 2 years