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23

抑制剂 & 化合物

2

天然产物

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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)。
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

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

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

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

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

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

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

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...

化合物

Linoleoyl Ethanolamide
Cat.No: T8425
Synonym:
Target: TRP/TRPV Channel
LY2183240
Cat.No: T15802
Synonym:
Target: FAAH, Autophagy
OMDM-1
Cat.No: T12302
Synonym: (Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide
Target: Endogenous Metabolite
ARN272
Cat.No: T5357
Synonym: ARN 272
Target: FAAH
OMDM-6
Cat.No: T12307
Synonym:
Target: Cannabinoid Receptor, Endogenous Metabolite, TRP/TRPV Channel
OMDM-5
Cat.No: T12306
Synonym:
Target: Cannabinoid Receptor, Endogenous Metabolite, TRP/TRPV Channel
URB937
Cat.No: T8646
Synonym:
Target: FAAH
MAFP
Cat.No: T15948
Synonym: Methyl Arachidonyl Fluorophosphonate
Target: Phospholipase
BIA 10-2474
Cat.No: T3354
Synonym: BIA10-2474
Target: FAAH, Autophagy
OMDM-3
Cat.No: T12304
Synonym:
Target: Others
OMDM-2
Cat.No: T12303
Synonym:
Target: Others
OMDM-4
Cat.No: T12305
Synonym:
Target: Others
MM-22
Cat.No: T23006
Synonym:
Target: Others
O-2093
Cat.No: T23100
Synonym:
Target: Others
VDM 11
Cat.No: T23503
Synonym:
Target: Others
Prostaglandin D2 Ethanolamide
Cat.No: T38389
Synonym: Prostaglandin D2 Ethanolamide
Target:
LEI-301
Cat.No: T69577
Synonym:
Target:
JNJ-40355003
Cat.No: T27681
Synonym: JNJ40355003
Target:
AM404
Cat.No: T39281
Synonym:
Target:
1-Palmitoyl-2-linoleoyl PE
Cat.No: T37785
Synonym:
Target:
Glycerophospho-N-Arachidonoyl Ethanolamine
Cat.No: T37530
Synonym:
Target:
CAY10412
Cat.No: T37684
Synonym: CAY10412
Target:
N-Decanoyl p-Nitroaniline
Cat.No: T37217
Synonym:
Target:
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

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...

天然产物

Anandamide
Cat.No: T14046
Synonym: 花生四烯酸乙醇胺,(5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide
Target: Cannabinoid Receptor, Endogenous Metabolite
N-Palmitoyl Glycine
Cat.No: T37219
Synonym:
Target:
TargetMol Loading
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