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10

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
T41350 6-Bromopravadoline

WIN 54461

Cannabinoid Receptor GPCR/G Protein
6-Bromopravadoline (WIN 54461) (WIN 54461) 是CB1受体的拮抗剂。6-Bromopravadoline 作为 [3H]Win 55212-2 的结合抑制剂 (IC50=515 nM),反映了其与大麻素受体结合。
T8511 TM38837

Cannabinoid Receptor GPCR/G Protein
TM38837 是外周选择性大麻素受体1型受体拮抗剂。它减少精神病副作用的倾向。它对大脑的渗透率有限,以降低或防止 CNS 不良反应,并保留潜在的抗肥胖作用。
T68500 AZD-2207

AZD-2207 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes mellitus and obesity.
T68515 AZD-1175

AZD-1175 is a cannabinoid receptor CB1 antagonist and highly lipophilic compound for the treatment of type 2 diabetes and obesity.
T78674 Isopropyl dodec-11-enylfluorophosphonate

IDEFP

FAAH Metabolism; Neuroscience
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) 为有机磷酯类化合物,能抑制中枢大麻素受体 (cannabinoid receptor) (CB1) 并具有相似的效力抑制FAAH(IC50s = 2 nM)。
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。
T38199 (±)-WIN 55,212 (mesylate)

(±)-WIN 55,212-2 is a potent aminoalkylindole cannabinoid (CB) receptor agonist with a Ki value of 62.3 and 3.3 nM for human recombinant central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, respectively. In contrast, the enantiomer (-)-WIN 55,212-3 acts a partial inverse agonist at CB1 (pIC50 = 5.5) and as a competitive neutral antagonist of CB2, reversing the inverse agonism evoked by SR 144528 (pEC50 = 5.3). (+)-WIN 55,212 (mesylate) is a mixture of the two enantiomers, (+)-WI...
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。
T35468 (±)19(20)-EDP Ethanolamide

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-...

化合物

CB1 antagonist 2
Cat.No: T14881
Synonym: AM4113
Target: Cannabinoid Receptor
6-Bromopravadoline
Cat.No: T41350
Synonym: WIN 54461
Target: Cannabinoid Receptor
TM38837
Cat.No: T8511
Synonym:
Target: Cannabinoid Receptor
AZD-2207
Cat.No: T68500
Synonym:
Target:
AZD-1175
Cat.No: T68515
Synonym:
Target:
Isopropyl dodec-11-enylfluorophosphonate
Cat.No: T78674
Synonym: IDEFP
Target: FAAH
(S)-SLV 319
Cat.No: T21914
Synonym:
Target:
(±)-WIN 55,212 (mesylate)
Cat.No: T38199
Synonym:
Target:
O-2050
Cat.No: T23099
Synonym:
Target: Others
(±)19(20)-EDP Ethanolamide
Cat.No: T35468
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1465 Cannabigerol

NOS; 5-HT Receptor; ROS GPCR/G Protein; Immunology/Inflammation; Neuroscience
Cannabigerol 是一种植物大麻素,是一种高亲和力 α2-肾上腺素能受体激动剂、中度亲和力 5-HT1A 受体拮抗剂和低亲和力 CB1/CB2受体拮抗剂。它可降低眼压,有潜力治疗青光眼。
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。

天然产物

Cannabigerol
Cat.No: TN1465
Synonym:
Target: NOS, 5-HT Receptor, ROS
Tetrahydrocannabivarin
Cat.No: TN5131
Synonym: THCV,delta9-Tetrahydrocannabivarin,CRM,Tetrahydrocannavarin
Target: Cannabinoid Receptor
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