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30

抑制剂 & 化合物

2

天然产物

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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。
T14881	CB1 antagonist 2 AM4113	Cannabinoid Receptor	GPCR/G Protein
	CB1 antagonist 2 (AM4113) 是一种 caimabinoid 1 拮抗剂，在体内抑制 CB1 的IC50值为 25.5 nM。
T13080L	Taranabant MK-0364	Cannabinoid Receptor	GPCR/G Protein
	Taranabant (MK-0364) 是一种具有选择性和高效性的 cannabinoid 1 (CB1) 受体反向激动剂，可用于研究肥胖和尼古丁依赖。
T28468	PSNCBAM-1 PSNCBAM 1	Cannabinoid Receptor	GPCR/G Protein
	PSNCBAM-1 (PSNCBAM 1) 是一种 CB1 受体负变构调节剂 (EC50 = 0.1 μM)，在体内具有吞噬作用。 PSNCBAM-1 可用于肥胖研究。
T9466	RTICBM-189	Others	Others
	RTICBM-189 是可透过血脑屏障的大麻素 1 型受体变构调节剂，在 Ca2+动员试验中pIC50为 7.54，对 hCB1和 mCB1的 pIC50分别为 5.29 和 6.25。
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。
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。
T10510	CB1 antagonist 1	Cannabinoid Receptor	GPCR/G Protein
	CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular.
T61849	AM8936
	AM8936 is a well-balanced and highly potent agonist for the cannabinoid receptor type-1 (CB1) in functional assays, with EC50 values of 8.6 nM and 1.4 nM for the rat CB1 (rCB1) and human CB1 (hCB1) receptors, respectively. It demonstrates a strong affinity for the rat CB1 receptor, exhibiting a K i value of 0.55 nM. In vivo studies have confirmed that AM8936 is a powerful and effective agonist for the CB1 receptor. Due to its therapeutic potential, AM8936 is particularly valuable for research fo...
T62180	CB1/2 agonist 2
	CB1/2 agonist 2 (compound 23) 是一种有效的非选择性大麻素 (cannabinoid) 配体，其Ki 分别为 3.5 nM 和 1.2 nM。CB1/2 agonist 2 是一种 CB1 的完全激动剂，也是 CB2 竞争性反向激动剂。CB1/2 agonist 2 表现出抗伤害效果。
T83533	(R)-Monlunabant (R)-MRI-1891	Cannabinoid Receptor	GPCR/G Protein
	(R)-Monlunabant ((R)-MRI-1891)为CB1受体调节剂，应用于肥胖及代谢病研究领域。
T61609	CB1-IN-2
	CB1-IN-2 (Compound 4g) is a potent and selective inhibitor of the CB1 receptor, exhibiting an IC50 value of 0.644 μM. This compound possesses the ability to penetrate the blood-brain barrier and has the potential to induce central nervous system (CNS) side effects similar to Rimonabant [1].
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...
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 ...
T69740	AMG-315
	AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a ...
T21914	(S)-SLV 319
	Ibipinabant (SLV319) 是一种有效，选择性和具有口服活性的大麻素 CB1 受体 (cannabinoid CB1 receptor) 的拮抗剂，Ki 值为 7.8 nM。Ibipinabant 对 CB1 的选择性超过 CB2 (Ki=7943 nM) 的 1000 倍以上。Ibipinabant 可用于肥胖和糖尿病的研究。
T75799	Hemopressin(human, mouse) TFA	Cannabinoid Receptor	GPCR/G Protein
	Hemopressin TFA，一种衍生自血红蛋白α1链的九肽，最初自大鼠脑匀浆分离。作为口服活性且选择性的CB1大麻素受体反向激动剂，Hemopressin TFA在炎性疼痛模型中具有抗伤害感受效应。
T38223	N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide
	N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide binds to the cannabinoid 1 (CB1) receptor with a Ki value of 365 nM in a radioligand binding assay using rat brain homogenate. It has an EC50 value of 698 nM for the peroxisome proliferator-activated receptor α (PPARα) in a luciferase reporter assay and, in rats, it decreases food intake. It does not inhibit fatty acid amide hydrolase (FAAH).
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。
T36591	ABD459
	ABD459 is a neutral antagonist of the central cannabinoid 1 (CB1) receptor (Ki = 8.6 nM). It inhibits food consumption in nonfasted mice without affecting motor activity. ABD459 reduces active food seeking for 5-6 hours after treatment, with no rebound after washout. ABD459 also diminishes rapid eye movement (REM) sleep, with no alterations of wakefulness or non-REM sleep.
T21811	LH 21
	LH-21 是一种有效的体内中性大麻素 CB1受体拮抗剂。LH-21 会导致剂量依赖性进食抑制，减少肥胖 Zucker 大鼠的食物摄入和体重增加。
T38049	Glycerophospho-N-Palmitoyl Ethanolamine
	N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. For example, arachidonoyl ethanolamide (AEA) is an endogenous neurotransmitter that evokes cellular responses by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). The different types of NAE are derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-palmitoyl ethanolamine (GP-NPEA) is the metabo...
T75798	Hemopressin(rat) TFA
	Hemopressin(rat) TFA，一种衍生自α1-珠蛋白九肽，最初分离自大鼠脑匀浆。该化合物通过口服能有效选择性地作为CB1大麻素受体的反向激动剂，并在炎性疼痛模型中表现出抗伤害感受活性。
T10294	AM9405	5-HT Receptor	GPCR/G Protein; Neuroscience
	AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩，IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动.
T78949	AM841	Cannabinoid Receptor	GPCR/G Protein
	AM841是一种高亲和力的亲电子配体，能与CB1大麻素受体中第六螺旋的半胱氨酸发生共价作用并激活该受体。此外，AM841能减少Forskolin刺激下的cAMP积累，并且减缓胃肠蠕动。
T1519L	Rimonabant SR141716,利莫那班	Cannabinoid Receptor; Antibacterial; Acyltransferase	GPCR/G Protein; Metabolism; Microbiology/Virology
	Rimonabant (SR141716) 是一种选择性的、能透过血脑屏障的中心大麻素受体 1 拮抗剂， Ki 值为 1.8 nM。它也能够抑制分枝杆菌膜蛋白 3。
T27809	LEI-101
	LEI-101 是有效的、选择性的、具有口服活性的大麻素CB2受体激动剂。LEI-101对 hCB2 的 pEC50值为 8，对 hERG 的 pKi 值小于 4。LEI-101 与 CB2 受体的结合能力比 CB1 强100 倍。LEI-101 具有炎症及氧化应激相关疾病的治疗潜力。
T35786	O-7460
	In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-depe...
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。
T37374	URB754
	URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fa...

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

CB1 antagonist 2

Cat.No: T14881

Synonym: AM4113

Target: Cannabinoid Receptor

Cat.No: T13080L

Synonym: MK-0364

Target: Cannabinoid Receptor

Cat.No: T28468

Synonym: PSNCBAM 1

Target: Cannabinoid Receptor

Cat.No: T9466

Target: Others

Cat.No: T36520

Target: Cannabinoid Receptor, GABA Receptor

Linoleoyl Ethanolamide

Cat.No: T8425

Target: TRP/TRPV Channel

CB1 antagonist 1

Cat.No: T10510

Target: Cannabinoid Receptor

Cat.No: T61849

CB1/2 agonist 2

Cat.No: T62180

(R)-Monlunabant

Cat.No: T83533

Synonym: (R)-MRI-1891

Target: Cannabinoid Receptor

Cat.No: T61609

Cat.No: T38204

Cat.No: T38138

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

Cat.No: T69740

Cat.No: T21914

Hemopressin(human, mouse) TFA

Cat.No: T75799

Target: Cannabinoid Receptor

N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide

Cat.No: T38223

Cat.No: T78083

Target: Cannabinoid Receptor

Cat.No: T36591

Cat.No: T21811

Glycerophospho-N-Palmitoyl Ethanolamine

Cat.No: T38049

Hemopressin(rat) TFA

Cat.No: T75798

Cat.No: T10294

Target: 5-HT Receptor

Cat.No: T78949

Target: Cannabinoid Receptor

Cat.No: T1519L

Synonym: SR141716,利莫那班

Target: Cannabinoid Receptor, Antibacterial, Acyltransferase

Cat.No: T27809

Cat.No: T35786

Cat.No: T23099

Target: Others

Cat.No: T37374

Cat. No.	Product Name	Target	Signaling Pathways
TN5131	Tetrahydrocannabivarin THCV,delta9-Tetrahydrocannabivarin,CRM,Tetrahydrocannavarin	Cannabinoid Receptor	GPCR/G Protein
	Tetrahydrocannabivarin (CRM) 是 cannabinoid type 1 receptor 的中性拮抗剂，对 2 型糖尿病有潜在治疗价值。
T11834	Leelamine hydrochloride	Others	Others
	Leelamine hydrochloride, a tricyclic diterpene extracted from pine tree bark, inhibits the transcriptional activity of the androgen receptor, known to regulate fatty acid synthesis [2,3]. This compound acts as a cannabinoid receptor type 1 (CB1) agonist and suppresses SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells, irrespective of androgen receptor status.

天然产物

Tetrahydrocannabivarin

Cat.No: TN5131

Synonym: THCV,delta9-Tetrahydrocannabivarin,CRM,Tetrahydrocannavarin

Target: Cannabinoid Receptor

Leelamine hydrochloride

Cat.No: T11834

Target: Others

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