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GW405833 盐酸盐

GW405833 盐酸盐用途

GW-405833(L768242)是一种有效的选择性大麻素受体2(CB2)激动剂,EC50为50.7 nM。GW-405833还表现为非竞争性CB1拮抗剂。GW-405833抑制炎症和神经病理性疼痛[1][2]。

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GW405833 盐酸盐名称

[ CAS 号 ]:
180002-83-9

[ 中文名 ]:
GW405833 盐酸盐

[ 英文名 ]:
L-768242

[中文别名 ]:

[英文别名 ]:

hms3268p12

GW405833 盐酸盐生物活性

[ 描述 ]:

GW-405833(L768242)是一种有效的选择性大麻素受体2(CB2)激动剂,EC50为50.7 nM。GW-405833还表现为非竞争性CB1拮抗剂。GW-405833抑制炎症和神经病理性疼痛[1][2]。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 大麻素受体

[ 靶点 ]

CB2:50.7 nM (EC50)

CB1:16.1 μM (EC50)

[参考文献]

[1]. Li AL, et al. Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther. 2017 Aug;362(2):296-305.

[2]. Li J, et al. Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation. Medchemcomm. 2019 Sep 17;10(11):1935-1947.

GW405833 盐酸盐物理化学性质

[ 熔点 ]:
47-49°C(lit.)

[ 分子式 ]:
C₂₃H₂₄Cl₂N₂O₃

[ 分子量 ]:
447.35

[ 精确质量 ]:
446.11600

[ PSA ]:
43.70000

[ LogP ]:
4.76620

[ 外观性状 ]:
固体

[ 储存条件 ]:
2-8°C

GW405833 盐酸盐安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H413

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ 海关编码 ]:
2934999090

GW405833 盐酸盐海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

GW405833 盐酸盐文献

Cannabinoids inhibit energetic metabolism and induce AMPK-dependent autophagy in pancreatic cancer cells.

Cell Death Dis. 4 , e664, (2013)

The anti-tumoral effects of cannabinoids have been described in different tumor systems, including pancreatic adenocarcinoma, but their mechanism of action remains unclear. We used cannabinoids specif...

Gemcitabine/cannabinoid combination triggers autophagy in pancreatic cancer cells through a ROS-mediated mechanism.

Cell Death Dis. 2 , e152, (2011)

Gemcitabine (GEM, 2',2'-difluorodeoxycytidine) is currently used in advanced pancreatic adenocarcinoma, with a response rate of < 20%. The purpose of our work was to improve GEM activity by addition o...

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