ag 10

AG-10 (Acoramidis) is an orally active and selective kinetic stabilizer of TTR (transthyretin). AG-10 exhibits activity for WT and V122I-TTR. AG-10 is used in the study of transthyretin amyloidosis.

AG 84-10 is similar to Angiotensinogen 6-13. It is a peptidic substrate analog. It also has antihypertensive effects.

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 microMAG hydrolysing activities in

Acoramidis hydrochloride (Alxn2060 hydrochloride) is an orally active and selective kinetic stabilizer of WT and V122I- TTR (transthyretin) . Acoramidis hydrochloride is used in the study for transthyretin amyloidosis.

(E)-AG 99 ((E)-Tyrphostin AG 99) is an EGFR kinase inhibitor with an IC50 of 10 μM in the human epidermoid carcinoma cell line A431.

Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4 6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

AG-012986 HCl is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4 6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 HCl showed antiproliferative activities in vitro with IC(50)s of <100 nmol L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

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......

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.