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Olorinab
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Olorinab图片
CAS NO:1268881-20-4
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议

产品名称
APD 371
产品介绍
Olorinab (APD 371) 是大麻素受体 2 型 (CB2) 强有效的、选择性的全激动剂,其对 hCB2 的EC50 值为 6.2 nM。

产品描述

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2.

体外活性

A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed. Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling[1].

体内活性

Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). The analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors[1]. In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration.

Cas No.

1268881-20-4

分子式

C18H23N5O3

分子量

357.41

别名

APD 371

储存和溶解度

DMSO:180mg/mL (503.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years