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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T15802 |
LY2183240
|
FAAH; Autophagy | Autophagy; Metabolism; Neuroscience |
LY2183240 是大麻素摄取阻滞剂。它是内源性大麻素降解酶脂肪酸酰胺水解酶的有效共价抑制剂。它抑制脂肪酸酰胺水解酶 (FAAH) 活性,IC50 为12.4 nM。它也抑制其他几种脑丝氨酸水解酶,对 MAG 脂肪酶、bh6 和 KIAA1363 的 IC50分别为 5.3、0.09 和 8.2 nM。 | |||
T12302 |
OMDM-1
(Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide |
Endogenous Metabolite | Metabolism |
OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) 是有效选择性的代谢稳定 anandamide 细胞摄取抑制剂,Ki=为2.4 μM。 | |||
T5357 |
ARN272
ARN 272 |
FAAH | Metabolism; Neuroscience |
ARN272 是大麻素转运抑制剂的一种。 | |||
T12307 |
OMDM-6
|
Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
OMDM-6 是 TRPV1(EC50 = 75 nM) 和 CB1 (Ki = 3.2 μM) 的双重激动剂。 OMDM-6 抑制 anandamide 细胞摄取,Ki 为 7.0 μM。 | |||
T12306 |
OMDM-5
|
Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂,Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂,EC50为 75 nM,显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。 | |||
T15948 |
MAFP
Methyl Arachidonyl Fluorophosphonate |
Phospholipase | Metabolism |
MAFP (Methyl Arachidonyl Fluorophosphonate) 是选择性,针对活性位点,不可逆的 cPLA2 和 iPLA2 抑制剂。 MAFP 也是一种有效的不可逆的 anandamide amidase 抑制剂。 | |||
T8646 |
URB937
|
FAAH | Metabolism; Neuroscience |
URB937 是一种口服具有活性的、外周限制的FAAH 抑制剂,IC50=26.8 nM,可增加 anandamide 水平,但不能影响脑内 FAAH 水平 (无法透过血脑屏障)。 | |||
T27681 |
JNJ-40355003
JNJ40355003 |
Others | Others |
JNJ-40355003, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor, elevates the plasma levels of three fatty acid amides: anandamide, oleoyl ethanolamide, and palmitoyl ethanolamide, in the rat, dog, and cynomolgous monkey. | |||
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。 | |||
T12304 | OMDM-3 | Others | Others |
OMDM-3 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 16.6 μM). | |||
T12303 |
OMDM-2
|
Others | Others |
OMDM-2 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 3.0 μM). | |||
T12305 |
OMDM-4
|
Others | Others |
OMDM-4 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 17.7 μM). | |||
T23006 | MM-22 | Others | Others |
biotinylated anandamide analog acts as a probe for visualizing the accumulation and intracellular trafficking of anandamide | |||
T23100 | O-2093 | Others | Others |
anandamide uptake inhibitor | |||
T38389 |
Prostaglandin D2 Ethanolamide
Prostaglandin D2 Ethanolamide |
Others | Others |
Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of minia... | |||
T23503 |
VDM 11
|
Others | Others |
anandamide transport inhibitor | |||
T84534 |
Arachidonoyl-N-methyl amide
|
Others | Others |
Anandamide (AEA), an endogenous cannabinoid, interacts with both central (CB1) and peripheral (CB2) cannabinoid receptors. Its effects are concluded through the cellular uptake and enzymatic breakdown of its amide bond by fatty acid amide hydrolase. Arachidonoyl-N-methyl amide, an analog of anandamide, specifically targets the human CB1 receptor, displaying a binding affinity with a Ki of 60 nM. It completely inhibits rat glial gap junction intercellular communication at a concentration of 50 µM... | |||
T69577 |
LEI-301
|
Others | Others |
LEI-301 is a novel potent inhibitor for the PLAAT family members, reducing the NAE levels, including anandamide, in cells overexpressing PLAAT2 or PLAAT5. | |||
T39281 |
AM404
|
Others | Others |
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. | |||
T37785 |
1-Palmitoyl-2-linoleoyl PE
|
Others | Others |
Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids. | |||
T84549 |
CAY10455
SKM 4-45-1 |
Others | Others |
CAY10455, an analog of arachidonoyl ethanolamide (anandamide; AEA), is non-fluorescent extracellularly but exhibits bright fluorescence at 530 nm inside cells due to esterase-mediated cleavage. Its uptake by C6 glioma cells is competitively inhibited by AEA and its analogs, suggesting that CAY10455 and AEA utilize the same transporter. Conversely, CAY10455 also inhibits the uptake of tritiated AEA, further indicating competition for the AEA transporter. | |||
T37530 |
Glycerophospho-N-Arachidonoyl Ethanolamine
|
Others | Others |
N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. The different types of NAE can be derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-arachidonoyl ethanolamine is the precursor of arachidonoyl ethanolamide (AEA), also known as anandamide. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibit... | |||
T84550 |
AMC Arachidonoyl Amide
AMC-AA |
Others | Others |
Arachidonoyl amide (AMC-AA) is a fatty acid amide among several that serve to quantify fatty acid amide hydrolase (FAAH) activity. FAAH, with its relative lack of selectivity, processes various amide head groups beyond ethanolamine, the head group of its primary endogenous substrate, anandamide (AEA). The interaction of AMC-AA with FAAH leads to the liberation of fluorescent aminomethyl coumarin, which has an absorption peak at 360 nm and emission at 465 nm. This fluorescence release facilitates... | |||
T84523 |
O-Arachidonoyl glycidol
|
Others | Others |
O-Arachidonoyl glycidol(compound 1)是一种2-花生四烯酰甘油(2-AG)的类似物,能够抑制胞质中2-油酰甘油(2-OG)的水解作用,其IC50值为4.5 µM。此外,O-Arachidonoyl glycidol还能阻断膜组分中2-OG和大麻素的水解,其IC50值分别为19 µM和12 µM。 | |||
T37684 |
CAY10412
CAY10412 |
Others | Others |
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... | |||
T84543 |
Arachidoyl Ethanolamide
N-Arachidoylethanolamine |
Others | Others |
Arachidoyl ethanolamide, a saturated fatty acyl ethanolamide lacking classical (CB1/CB2) activity, plays a role in a complex system comprising central cannabinoid (CB1), peripheral cannabinoid (CB2), and non-CB receptor-mediated pharmacology. This system has paved the way for extensive research in diverse fields such as memory, weight loss and appetite, neurodegeneration, tumor surveillance, analgesia, and inflammation. Unlike other compounds, Arachidoyl ethanolamide does not bind to the murine ... | |||
T37217 |
N-Decanoyl p-Nitroaniline
|
||
N-Decanoyl p-nitroaniline (DepNA) is one of several nitroaniline fatty acid amides which can be used to measure fatty acid amide hydrolase (FAAH) activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate anandamide (AEA). It also will hydrolyze fatty acid amides with fewer carbons and fewer double bonds than arachidonate. Exposure of DepNA to FAAH activity results in the release of the yellow colori... | |||
T84547 |
PHOP
CAY10402 |
Others | Others |
Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 va... |
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。 | |||
T37219 |
N-Palmitoyl Glycine
|
Others | Others |
The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100... |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01325 |
FAAH2 Protein, Human, Recombinant (His)
Amidase domain-containing protein,Anandamide amidoh... |
Human | E. coli |
Catalyzes the hydrolysis of endogenous amidated lipids like the sleep-inducing lipid oleamide ((9Z)-octadecenamide), the endocannabinoid anandamide (N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-ethanolamine), as well as other fatty amides, to their corresponding fatty acids, thereby regulating the signaling functions of these molecules. Hydrolyzes monounsaturated substrate anandamide preferentially as compared to polyunsaturated substrates. FAAH2 Protein, Human, Recombinant (His) is expressed in E. coli e... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMIH-0620 |
Arachidonoyl Ethanolamide-d4
AEA-d4 |
||
Deuterated anandamide, a synthetically modified version of anandamide where hydrogen atoms are replaced with deuterium (D), exhibits enhanced stability against oxidative degradation. This modification conserves the compound's pharmacological properties while prolonging its shelf life and efficacy in research applications, particularly in analytical and biochemical studies to elucidate the complex mechanisms of the endocannabinoid system. |