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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-GW833972A
GW833972A

Chemical Structure : GW833972A

CAS No.: 1092502-33-4

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GW833972A (GW 833972A, GW-833972A)

货号: PC-26472Not For Human Use, Lab Use Only.

GW833972A is a potent, selective CB2 receptor agonist with pEC50 of 7.3 and 7.5 for human and rat CB2 receptors respecitvely, shows 1000-fold selectivity over CB1 receptor, also binds BMAL2 with high affinity and facilitates its protein degradation.

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2380 In stock
25 mg ￥3980 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GW833972A is a potent, selective CB2 receptor agonist with pEC50 of 7.3 and 7.5 for human and rat CB2 receptors respecitvely, shows 1000-fold selectivity over CB1 receptor, also binds BMAL2 with high affinity and facilitates its protein degradation.
GW833972A (0.3-300 uM) induced a concentration-dependent inhibition of the guinea-pig vagus nerve activity, stimulated by either capsaicin, hypertonic saline or PGE2.
GW833972A abolished Capsaicin-induced depolarizations at 300 μM with EC50 of 33.9 uM.
GW833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB2 receptor antagonist.
GW833972A reduced RAD51 expression, leading to an accumulation of DNA damage, decreased cell viability and reduced OCCC tumor growth.
GW833972A enhanced the effectiveness of Poly (ADP-ribose) polymerase inhibitor (PARPi) treatments in BMAL2-expressing OCCC.

物理化学性质&存储条件

分子量 444.24
分子式 C18H14Cl2F3N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((3-chlorophenyl)amino)-N-(pyridin-4-ylmethyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide hydrochloride

参考文献

1. Belvisi MG, et al. Br J Pharmacol. 2008 Oct;155(4):547-57.

2. Mlost J, et al. Biomed Pharmacother. 2021 Apr;136:111283.

3. Tan GYT, et al. EMBO Mol Med. 2026 Apr 3. doi: 10.1038/s44321-026-00414-8.

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