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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-AEF0117
AEF0117

Chemical Structure : AEF0117

CAS No.: 1610878-71-1

AEF0117 (AEF-0117, AEF 0117)

货号: PC-20950Not For Human Use, Lab Use Only.

AEF0117 (AEF-0117) is a potent, signaling-specific inhibitor of the cannabinoid receptor 1 (CB1), inhibits the decrease in cellular respiration induced by THC (1 µM) in HEK293 cells transfected with hCB1 with IC50 of 3 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AEF0117 (AEF-0117) is a potent, signaling-specific inhibitor of the cannabinoid receptor 1 (CB1), inhibits the decrease in cellular respiration induced by THC (1 µM) in HEK293 cells transfected with hCB1 with IC50 of 3 nM.
AEF0117 inhibited Δ9-tetrahydrocannabinol (THC)-induced p-ERK1/2 in both cell lines with similar potency (IC50 300 nM) in CHO-hCB1 cells, and STHdhQ7/Q7 cells (mouse CB1).
AEF0117 (15 µg/kg) significantly reduced intravenous (i.v.) self-administration of the CB1 agonist WIN55,212-2 in CD-1 Swiss male mice and of THC in male squirrel monkeys.
AEF0117 (15 µg/kg) also inhibited THC-induced increases in nucleus accumbens (Nac) extracellular dopamine (DA) in freely moving rat.
AEF0117 inhibited the effects of THC related to cannabis addiction in vivo.

物理化学性质&存储条件

分子量 436.64
分子式 C29H40O3
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

CC([C@H]1CC[C@@]2([H])[C@]3([H])CC=C4C[C@@H](OCC5=CC=C(OC)C=C5)CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O

参考文献

1. Margaret Haney, et al. Nat Med. 2023 Jun;29(6):1487-1499.

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