LY320135

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LY320135

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。

CAS NO:

176977-56-3

LY320135是一种有效的和选择性的CB1受体拮抗剂，K_i值为 141 nM。LY320135 还与5-HT₂和muscarinic receptors结合，K_i值分别为 6.4 μM 和 2.1 μM。LY320135具有神经保护作用。

生物活性

LY320135 is a potent and selective antagonist ofCB1receptor, with aK_iof 141 nM. LY320135 also binds to5-HT₂andmuscarinic receptorswithK_is of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect^[1]^[2].

IC₅₀& Target^[1]

CB1

141 nM (Ki)

5-HT₂Receptor

6.4 μM (Ki)

muscarinic receptor

2.1 μM (Ki)

CB2

>10 μM (Ki)

体外研究
(In Vitro)

LY320135 has a relatively low affinity for the CB2 receptor (K_i=14.9±0.4 μM) and ten other unrelated receptors^[1].
LY320135 (1 nM-10 μM) inhibits the anandamide-mediated forskolin-stimulated cAMP accumulation in CHO cell, with an IC₅₀of 734±122 nM^[1].
LY320135 (0.1-1000 nM; 1-8 min) can reverse calcium current (I_Ca) inhibition by WIN 55212-2 in N18 cells, with an IC₅₀of 55±10 nM^[1].
LY320135 (1 μM) prevents activation of K_ircurrent by WIN 55212-2 in AtT-20-CB1 cells^[1].
LY 320135 (0.001-1 μM) reduces CA1 injury induced by 20 min oxygen-glucose deprivation (OGD) in a concentration-dependent manner^[2].

分子量

383.40

Formula

C₂₄H₁₇NO₄

CAS 号

176977-56-3

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.