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CB1/2 agonist 4
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。
CB1/2 agonist 4图片
CAS NO:2772949-38-7
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CB1/2 agonist 4 是CB1完全激动剂和CB2部分激动剂，EC50值分别为 15.09 nM 和 1.16 nM。CB1/2 agonist 4 对 hCB1 和 hCB2 受体也有亲和力，Ki值分别为 1.1 nM 和 4.2 nM。CB1/2 agonist 4 具有明显的抗伤害感受活性，也可以激活大麻素和TRPV1受体，其IC50值为 0.8 μM,EC50值为 0.12 μM。
生物活性

CB1/2 agonist 4 is a fullCB1agonist andCB2partial agonist withEC50values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities withKivalues of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid andTRPV1receptor with values ofIC50andEC50is 0.8 μM and 0.12 μM, respectively[1].

IC50& Target

Ki: 1.1 nM (hCB1); 4.2 nM (hCB2)[1].
EC50: 15.09 nM (CB1); EC50: 1.16 nM (CB2)[1].
IC50: 0.8 μM, EC50: 0.12 μM (TRPV1)[1].

体外研究
(In Vitro)

CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Kivalues of 1.1 nM and 4.2 nM, respectively[1].
CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membranes with an EC50value of 15.09 nM[1].
CB1/2 agonist 4 (0.1 mM) is able to slightly stimulate [35S]GTPγS binding to hCB2-CHO cell membranes, behaving as a weak partial agonist to CB2 receptors of 1.16 nM[1].

体内研究
(In Vivo)

CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) has a stronger antinociceptive activity[1].
CB1/2 agonist 4 (1, 3 and 4 mg/kg, i.p.) can activate TRPV1 channel and it behaved as a good TRPV1 agonist with an IC50value of 0.8 μM and EC50value of 0.12 μM[1].

Animal Model:Male CD-1 outbred mice[1]
Dosage:1, 3 and 4 mg/kg
Administration:1, 3 and 4 mg/kg, i.p.
Result:Significantly reduced the late phase of formalin-induced nociceptive behaviour in a dose dependent manner and slightly decreased also the first phase of nociceptive response.
分子量

431.65

Formula

C27H45NO3

CAS 号

2772949-38-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.