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Cat. No. | Product Name | Target | Signaling Pathways |
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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)。 | |||
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)。 | |||
T15948 |
MAFP
Methyl Arachidonyl Fluorophosphonate |
Phospholipase | Metabolism |
MAFP (Methyl Arachidonyl Fluorophosphonate) (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。 | |||
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 | |||
T23503 |
VDM 11
|
Others | Others |
anandamide transport inhibitor | |||
T38389 |
Prostaglandin D2 Ethanolamide
Prostaglandin D2 Ethanolamide |
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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... | |||
T69577 |
LEI-301
|
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LEI-301 is a novel potent inhibitor for the PLAAT family members, reducing the NAE levels, including anandamide, in cells overexpressing PLAAT2 or PLAAT5. | |||
T27681 |
JNJ-40355003
JNJ40355003 |
||
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. | |||
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. | |||
T37785 |
1-Palmitoyl-2-linoleoyl PE
|
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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. | |||
T37530 |
Glycerophospho-N-Arachidonoyl Ethanolamine
|
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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... | |||
T37684 |
CAY10412
CAY10412 |
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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... | |||
T37217 |
N-Decanoyl p-Nitroaniline
|
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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... |
Cat. No. | Product Name | Target | Signaling Pathways |
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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
|
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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... |