LY320135 - CAS:176977-56-3

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LY320135 (Synonyms:[6-甲氧基-2-(4-甲氧基苯基)苯并[B]呋喃-3-基](4-氰基苯基)甲酮)

目录号 : KCM12010 CAS No. : 176977-56-3 纯度 : ≥98%

Data Sheet SDS 产品使用指南

LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Ks = 224 and >10,000 nM for CB and CB, respectively, in vitro). It is selective for CB over α- and α- adrenergic, D and D dopamine, benzodiazepine, histamine H, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; ) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB agonist CP 55,940 .

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1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT₂ and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.

体外研究

LY320135 has a relatively low affinity for the CB2 receptor (K_i=14.9±0.4 μM) and ten other unrelated receptors.
LY320135 (1 nM-10 μM) inhibits the anandamide-mediated forskolin-stimulated cAMP accumulation in CHO cell, with an IC₅₀ of 734±122 nM.
LY320135 (0.1-1000 nM; 1-8 min) can reverse calcium current (I_Ca) inhibition by WIN 55212-2 in N18 cells, with an IC₅₀ of 55±10 nM.
LY320135 (1 μM) prevents activation of K_ir current by WIN 55212-2 in AtT-20-CB1 cells.
LY 320135 (0.001-1 μM) reduces CA1 injury induced by 20 min oxygen-glucose deprivation (OGD) in a concentration-dependent manner.

分子式

C₂₄H₁₇NO₄

分子量

383.4

CAS号

176977-56-3

中文名称

4-[[6-甲氧基-2-(4-甲氧基苯基)-3-苯并呋喃]羰基]苯甲腈

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥98%

Data Sheet

SDS

产品使用指南

Felder CC, et, al. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther. 1998 Jan; 284(1):291-7.

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