2-ag

AG-1557 hydrochloride (189290-58-2(free base)) 是一种表皮生长因子受体 (EGFR) 酪氨酸激酶抑制剂 (pIC50: 8.194)。

AG-13958 (AG-013958) 是 VEGFR 酪氨酸激酶抑制剂，可用于年龄相关性黄斑变性 (AMD) 的脉络膜新生血管形成的研究。

Axitinib (AG-013736) 是一种多靶点酪氨酸激酶抑制剂，能够抑制 VEGFR1、VEGFR2、VEGFR3 和 PDGFRβ (IC50=4 20 0.4 2 nM)。Axitinib 具有抗肿瘤活性，用于肾细胞癌的治疗。

Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂，能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性，具有研究 AML 的潜力。

Repaglinide (AG-EE 623ZW) 是一种能够用于2 型糖尿病的胰岛素促分泌剂。

DO34 is a highly potent and centrally active inhibitor of diacylglycerol lipase (IC50: 6 nM for DAGLα conversion of SAG to 2-AG).

PP2 (AG 1879,AGL 1879) 是 Lck Fyn 抑制剂 (IC50:4 5 nM)，对 EGFR 的效力降低约 100 倍，对 ZAP-70、PKA 和 JAK2 无活性。

Tyrphostin AG1433 (AG1433) 是选择性的PDGFRβ和VEGFR-2 (Flk-1 KDR)抑制剂，IC50分别为 5.0 μM 和 9.3 μM。Tyrphostin AG1433有防止血管形成的活性。

Voreloxin hydrochloride (SNS-595 hydrochloride) 是一种新型拓扑异构酶 II 抑制剂，能够诱导 DNA 双链断裂，阻滞 G2 期，引起细胞凋亡。

KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂，其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。

AG-494 (Tyrphostin B48) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂，IC50为0.7 μM。它阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。它抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化，IC50为 1.1、39、45 和 6 μM。

MJN110 (Cravatt Reagent) 是选择性的、口服具有活性的单酰基甘油脂肪酶 (MAGL) 抑制剂，对 hMAGL 和 2-花生四烯酸甘油酯 (2-AG) 的IC50分别为 9.1 nM 和 2.1 nM。它具有阿片类药物保护作用，具有显著的抗痛觉过敏活性。

AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂，可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。

LEI-106, a novel potent sn-1 DAGLalpha inhibitor, blocks the hydrolysis of sn-1-oleoyl-2-AG, inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6.

OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM2-AG hydrolysing activities in

SAR-629 is an MGL inhibitor or 2-AG degradation inhibitor.

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 fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg/kg) decreases serum cholesterol levels and total bod......

Antagonist G TFA 作为后叶加压素（vasopressin）的有效拮抗剂，同时对GRP和缓激肽具有弱拮抗作用。此外，Antagonist G 能够诱导AG-1转录，增强癌细胞对化疗的敏感性。

2-Pyridineacetamide, 5-methylthio- is a biochemical.

AG 1295 是选择性血小板衍生生长因子受体酪氨酸激酶抑制剂。它能抑制 PDGFR 的自磷酸化，对 EGF 受体的自磷酸化无影响。

The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and FAAH with IC50 values of 0.8 and 3 nM, respectively. At 10 mg/kg, IDFP elevates brain levels of 2-AG and AEA more than 10-fold, and decreases levels of arachidonic acid by a similar magnitude.

2-Pyridineacetamide, 5-ethylthio- is a biochemical.

AG 1406 是受体酪氨酸激酶 VEGF 受体 2 的选择性抑制剂。

AG-120 (racemic) 是 AG-120 的外消旋混合物，是一种可口服的异柠檬酸脱氢酶 1 型 (IDH1) 抑制剂，具有潜在的抗肿瘤活性。

1-Arachidonoyl-d8-rac-glycerol (1-AG-d8) serves as an internal standard for 1-AG quantification via GC or LC-MS. As a weak CB1 receptor agonist, 1-AG exhibits potential pharmacological effects. Notably, 1-AG, an isomer of 2-AG, is more stable, avoiding the rapid in vitro and in vivo isomerization that diminishes 2-AG's cannabinergic efficacy due to conversion to 1-AG (also known as 1(3)-AG), a common impurity in synthetic 2-AG formulations.

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

JNJ-42226314 是一种具有高选择性的非共价单酰基甘油脂肪酶 (MAGL) 抑制剂，具有抗伤害作用。JNJ-42226314 通过内源性大麻素-2-丙烯酰甘油（2-AG）在神经病理性疼痛和炎症性疼痛模型中显示出疗效。

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。

JZL 184 是不可逆的、选择性的MAGL 抑制剂，对MAGL 的选择性比 FAAH 高 300 倍以上。它可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。

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-dependently inhibit high-fat diet intake and reduce body weight.

Enasidenib (AG-221) 是口服具有活力的、可逆的、选择性IDH2突变酶抑制剂，抑制IDH2R140Q 和 IDH2R172K 的IC50分别为100 和 400 nM。

2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an entourage effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.

AG-28262 besylate is a VEGFR-2 Inhibitorwhich may affect alanine aminotransferase gene expression and enzymatic activity in the liver.

2-Arachidonoylglycerol (2-AG) is identified as a more potent endogenous cannabinoid ligand compared to its analogue, 1-Arachidonoylglycerol (1-AG), exhibiting 10 to 100 times the ligand binding affinity and agonist activity at the CB1 receptor, thus making it a natural ligand. However, 2-AG's chemical instability leads to rapid isomerization to 1-AG (also referred to as 1(3)-AG) both in vitro and in vivo. This isomerization process, where 1-AG becomes a frequent contaminant in synthetic 1-AG preparations, significantly decreases their cannabinergic potency. Furthermore, 1-AG is characterized as a weak CB1 receptor agonist with potential for other pharmacological effects.

2-arachidonyl glycerol (2-AG) exhibits cannabinoid (CB) agonist activity at the CB1 receptor, is an important endogenous monoglyceride species, and is thus considered to be the natural ligand for the CB1 receptor. 2-AG can also be metabolized by cyclooxygenase-2 and specific prostaglandin H2 (PGH2) isomerases to form PG 2-glyceryl esters. Fluprostenol serinol amide (Flu-SA) is a stable analog of PGF2α 2-glyceryl ester that has much greater stability. The biological activity of Flu-SA has not yet been determined.