Lemborexant (E-2006) 是一种 orexin OX1 和 OX2 受体的可逆，竞争性和口服活性双重拮抗剂，IC₅₀ 值分别为 6.1 nM 和 2.6 nM。Lemborexant 有潜力用于失眠的研究。

Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC 50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia.

Solid

OX1 6.1 nM (IC50) OX2 2.6 nM (IC50

A high-fat and high-calorie meal has been found to delay the time to peak levels by 2 hours. Its plasma protein binding in vitro is 94%. Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5. has not independently confirmed the accuracy of these methods. They are for reference only.

Lemborexant is administered orally to pregnant rats during the period of organogenesis in 2 studies at doses of 60, 200, and 600 mg/kg/day or 20, 60, and 200 mg/kg/day, which are approximately 6 to >300 times the maximum recommended human dose (MRHD) based on AUC. Lemborexant causes maternal toxicity, manifests by decreased body weight and food consumption, decreases mean fetal body weight, an increased number of dead fetuses, and skeletal, external and visceral malformations (omphalocele, cleft palate, and membranous ventricular septal defect) at >300 times the MRHD based on AUC.
Lemborexant causes maternal toxicity that consisted of decreased body weight and food consumption and toxicity to offspring consisting of decreased pup body weights, decreases femur length, and decreases acoustic startle responses at 206 times the MRHD based on AUC.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. OREXIN RECEPTOR ANTAGONIST PROVEN EFFECTIVE FOR BOTH SLEEP ONSET AND SLEEP MAINTENANCE IN CLINICAL DEVELOPMENT PROGRAM OF MORE THAN 2,000 PATIENTS. 2019.
[2]. HIGHLIGHTS OF PRESCRIBING INFORMATION

In Vitro: DMSO : 100 mg/mL (243.65 mM; Need ultrasonic)配制储备液