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Cat. No. | Product Name | Target | Signaling Pathways |
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T9687 |
MAGL-IN-4
His121 ARG57 |
Lipase | Metabolism |
MAGL-IN-4 (His121 ARG57) 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂,IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。 | |||
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。 | |||
T3354 |
BIA 10-2474
BIA10-2474 |
FAAH; Autophagy | Autophagy; Metabolism; Neuroscience |
BIA 10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂,与人类内源性大麻素系统相互作用,可增加中枢神经系统和外周组织,对大鼠大脑不同区域的 IC50值为50至70mg/kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。 | |||
T23494 |
UCM 707
|
Others | Others |
endocannabinoid transport inhibitor | |||
T69899 |
WOBE437
|
||
WOBE437 is a selective endocannabinoid reuptake inhibitor which reduces disease progression in a mouse model of multiple sclerosis | |||
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 ... | |||
T37684 |
CAY10412
CAY10412 |
||
Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for... | |||
T39281 |
AM404
|
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AM404 is a chemical compound that functions as an inhibitor of endocannabinoid reuptake. It effectively blocks the transport of anandamide, with IC50 values measured in the low micromolar range. Moreover, AM404 exhibits the ability to induce relaxation in rat isolated hepatic arteries contracted with Phenylephrine. This relaxation effect is quantified by a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 μM). Additionally, AM404 possesses a neuroprotective effect. | |||
T77212 | L-α-lysophosphatidylinositol (Soy) (sodium) | ||
L-α-lysophosphatidylinositol Soy sodium 作为GPR55的内源性配体,是一种既属于内源性溶血磷脂也是内源性大麻素神经递质的化合物。 | |||
T60957 |
Palmitoyl serinol
|
||
Palmitoyl serinol (N-Palmitoyl serinol) 是内源性大麻素 N-棕榈酰乙醇胺(PEA) 的类似物,可改善正常和发炎皮肤的表皮通透性屏障。 | |||
T36065 |
N-Oleoyl-L-Serine
|
||
Bone mass and shape is continuously remodeled by the concerted and balanced action of osteoblasts (bone forming cells) and osteoclasts (bone-resorbing cells). The endocannabinoid system plays an essential role in the maintenance of normal bone mass via signaling through the CB2 receptor. N-Oleoyl-L-serine is an endogenous lipid that has been reported to stimulate bone formation and to inhibit bone resorption. | |||
T64371 |
Virodhamine
O-arachidonoyl ethanolamine |
Cannabinoid Receptor | GPCR/G Protein |
Virodhamine (O-arachidonoyl ethanolamine) 是一种内源性大麻素,是CB1受体的拮抗剂和CB2受体的激动剂。Virodhamine 可用于阿尔茨海默病等神经系统疾病的研究。 | |||
T35408 |
(±)10(11)-EDP Ethanolamide
|
||
(±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively). It is produced though direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. 10,11-EDP epoxide (12.5 and 25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It induces apoptosis and inhibits cell migration in a wound-healing assay in 143B, MG63, and HOS osteosarcoma cells. (±)10(... | |||
T35786 |
O-7460
|
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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... | |||
T75022 | JZP-MA-11 | ||
JZP-MA-11是一种用于正电子发射断层扫描(PET)的配体,专一性靶向内源性大麻素α/β-水解酶结构域6(ABHD6)酶,并具有126 nM的IC50值,表明其对ABHD6有选择性抑制作用。JZP-MA-11能有效穿过血脑屏障(BBB)。[18F]JZP-MA-11展现出在靶向小鼠及非人灵长类(NHP)大脑ABHD6方面的临床前评估潜力。 | |||
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-... | |||
T70882 |
Orlistat-d3
|
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Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14046 |
Anandamide
花生四烯酸乙醇胺,(5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide |
Cannabinoid Receptor; Endogenous Metabolite | GPCR/G Protein; Metabolism |
Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide) 是一种免疫调节剂,通过大麻素受体 CB1 和 CB2 起作用,还通过中枢神经系统中的其他靶点起作用,如 GPR18/GPR55。 | |||
TN3575 |
(±)-Cannabichromene
Cannabichromene,大麻色原烯,Cannabichrome |
Cannabinoid Receptor | GPCR/G Protein |
(±)-Cannabichromene 是一种发现于大麻的 2,2-dimethyl-2H-chromene 衍生物。 |