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14

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T5996	CB1-IN-1 DBPR211,1-(2,4-二氯苯基)-N-1-哌啶基-4-[[(1-吡咯烷基磺酰基)氨基]甲基]-5-[5-[2-[4-(三氟甲基)苯基]乙炔基]-2-噻吩基]-1H-吡唑-3-甲酰胺	Cannabinoid Receptor	GPCR/G Protein
	CB1-IN-1 (DBPR211) 是新型的外周大麻素-1受体 (CB1R) 拮抗剂，作用于CB1R (EC50 = 3 nM) 和 CB2R 的Ki 分别为0.3 nM 和 21 nM。
T10697	CB2R-IN-1	Others	Others
	CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).
T30252	AZD1940 UNII-0J0035E9FT,AZD-1940,AZD 1940	Cannabinoid Receptor	GPCR/G Protein
	AZD1940 (UNII-0J0035E9FT)是一种高亲和力的大麻素CB(1)/CB(2)受体激动剂，具有口服活性，应用于口面疼痛的研究。
T8425	Linoleoyl Ethanolamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Linoleoyl ethanolamide 是脂肪酸乙醇酰胺。它可弱结合 CB1 和 CB2 受体，并分别抑制[3H]CP-55,940的结合，Ki 分别为 10 和 25μM。它在引起小鼠过氧化氢酶方面的效力是 anandamide 的4倍，且对睡眠时间无延长效果。
T4654	(±)-Ibipinabant (±)-BMS6462,SLV319,(±)-SLV319	Cannabinoid Receptor	GPCR/G Protein
	(±)-Ibipinabant ((±)-SLV319) 是一种有效选择性的大麻素-1 (CB-1) 受体拮抗剂，IC50=22 nM。(±)-SLV319 是 SLV319的消旋体。
T36520	COR659	Cannabinoid Receptor; GABA Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。
T23099	O-2050	Others	Others
	O-2050 是一种高亲和力的大麻素CB1受体拮抗剂，Ki 为 2.5 nM。O-2050 抑制大麻素 CB2受体，Ki 为 0.2 nM。O-2050 减少了小鼠的食物摄入量，并且引起小鼠运动。
T61336	Numidargistat dihydrochloride
	Numidargistat dihydrochloride (CB-1158) is a highly potent and orally active chemical compound that effectively inhibits arginase. It exhibits IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride contributes to immuno-oncology, making it a valuable agent in the field [1].
T78083	CB-25	Cannabinoid Receptor	GPCR/G Protein
	CB-25是一种CB1大麻素受体的部分激动剂配体。它能增强Forskolin诱导的癌细胞中cAMP的形成，但在Forskolin诱导的hCB1-CHO细胞中则不显示增强作用。
T39309	Telaglenastat hydrochloride CB-839 hydrochloride
	Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.
T28235	OMDM169 OMDM 169,OMDM-169
	OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM<IC(50)<0.41 microM towards 2-AG hydrolysing activities in
T38028	(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide
	N-Acyl ethanolamines (NAEs) have diverse biological actions that are strongly affected by the associated acyl group. Docosahexaenoyl ethanolamide (DHEA) has potential signaling roles in cancer, inflammation, and neurological development and functioning. At least some of DHEA's effects are mediated through cannabinoid (CB) receptors, while some NAEs also act as vanilloid receptor agonists and voltage-gated K+ channel blockers. (R)-(+)-Docosahexaenyl-1'-hydroxy-2'-propylamide is a homolog of DHEA,...
T38138	ACEA 2'-chloro-AEA,Arachidonoyl 2'-Chloroethylamide
	Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in ...
T38204	GAT229
	GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 an...

化合物

Cat.No: T5996

Synonym: DBPR211,1-(2,4-二氯苯基)-N-1-哌啶基-4-[[(1-吡咯烷基磺酰基)氨基]甲基]-5-[5-[2-[4-(三氟甲基)苯基]乙炔基]-2-噻吩基]-1H-吡唑-3-甲酰胺

Target: Cannabinoid Receptor

Cat.No: T10697

Target: Others

Cat.No: T30252

Synonym: UNII-0J0035E9FT,AZD-1940,AZD 1940

Target: Cannabinoid Receptor

Linoleoyl Ethanolamide

Cat.No: T8425

Target: TRP/TRPV Channel

(±)-Ibipinabant

Cat.No: T4654

Synonym: (±)-BMS6462,SLV319,(±)-SLV319

Target: Cannabinoid Receptor

Cat.No: T36520

Target: Cannabinoid Receptor, GABA Receptor

Cat.No: T23099

Target: Others

Numidargistat dihydrochloride

Cat.No: T61336

Cat.No: T78083

Target: Cannabinoid Receptor

Telaglenastat hydrochloride

Cat.No: T39309

Synonym: CB-839 hydrochloride

Cat.No: T28235

Synonym: OMDM 169,OMDM-169

(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide

Cat.No: T38028

Cat.No: T38138

Synonym: 2'-chloro-AEA,Arachidonoyl 2'-Chloroethylamide

Cat.No: T38204

Cat. No.	Product Name	Target	Signaling Pathways
T5S1897	Linderalactone	Apoptosis; Others; JAK	Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells
	Linderalactone 是从乌药中分离出来的一种倍半萜烯内酯，通过调节凋亡相关蛋白的表达和抑制 JAK/STAT 信号通路来抑制癌细胞生长。它以 IC50值为 15 µM 来抑制肺癌 A-549 细胞的增殖。

天然产物

Cat.No: T5S1897

Target: Apoptosis, Others, JAK

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