glp

EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.

UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

GLP-1R Agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).

GLP-1(32-36)amide acetate is a pentapeptide and derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide acetate could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice.

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of 64.5 nM, and is utilized in diabetes treatment research.

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools. GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1

GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).

GLP-1 Receptormodulator 1 (Compound 7) is an effective positive allosteric modulator of the GLP-1 receptor. It is utilized in the research of obesity and type 2 diabetes.

Compound 1, also known as GLP-1R agonist 26, is an agonist of the glucagon-like peptide-1 receptor (GLP-1R) with an EC50 of <10 nM.

GLP-1R agonist 27 (compound 21) is a potent and orally active GLP-1R agonist. It enhances the accumulation of cyclic adenosine monophosphate (cAMP), reduces blood glucose levels, and decreases food intake. GLP-1R agonist 27 shows potential for research in obesity and type 2 diabetes mellitus (T2DM).

GLP-1 receptoragonist 16 (Example 53) is a GLP-1 agonist applicable for research in diabetes, obesity, or diseases related to non-alcoholic steatohepatitis.

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist that enhances insulin secretion and is applicable for research into GLP-1R-related disorders.

GLP-1R agonist 29 (Compound 20) is a GLP-1R agonist that induces hGLP-1R-mediated cAMP stimulation with an EC50 of 0.018 nM. It exhibits favorable pharmacokinetic properties and shows good in vivo exposure, with an AUC0-∞,sc of 77688 ng·h/mL.

GLP-1 receptor agonist 17-d3 (Compound 701) is the deuterated form of GLP-1R agonist 17, which acts as a GLP-1 receptor agonist and is applicable in cardiovascular and metabolic disease research.

GLP-1R agonist 30 is an orally active, selective GLP-1R agonist with an EC50 of 0.048 nM. It exhibits outstanding selectivity, with EC50 values exceeding 20 μM for GLP-2R, GIPR, and GCPR. GLP-1R agonist 30 significantly enhances cAMP stimulation and reduces hERG inhibition. The compound has good absorption and excellent β-arrestin pathway selectivity. Additionally, GLP-1R agonist 30 improves glucose tolerance and promotes insulin secretion in B-hGLP1R gene knock-in mice.

GLP-1R agonist 21 (Compound I-134) is an agonist of the glucagon-like peptide-1 receptor (GLP-1 receptor) with an EC50 of 0.0104 nM.

GLP-1R agonist 22 (Compound I-135) functions as an agonist for the glucagon-like peptide-1 receptor (GLP-1 receptor), with an EC50 of 0.0165 nM.

GLP-1R agonist 20 (Compound I-132) is an agonist of the glucagon-like peptide-1 receptor (GLP-1 receptor), with an EC50 value of 0.0162 nM.