gp 2

CGP 20712 A (CGP 20712 mesylate) is a selective and potent β1-adrenergic receptor antagonist (IC50: 0.7 nM) with antihypertensive activity, capable of reversing RKT-induced gastric relaxation.

CGP 20376 is a benzothiazole compound, an anthelmintic, with dual dose-dependent modulation of in vitro effects on the respiratory burst of eosinophils and antifibrillatory properties.

CGP 29030A is a new piperazine derivative with analgesic activity and significant inhibitory effect on potentially nociceptive dorsal horn neurons, which can be used to study painful disorders.

P-gp modulator 2 (Compound 27) is a potent competitive and metabotropic modulator of P-glycoprotein (P-gp).

P-gp Inhibitor 2 is a powerful P-glycoprotein (P-gp) inhibitor, effective in reversing Doxorubicin resistance with an IC50 of 0.22 µM in human colorectal carcinoma cells overexpressing P-gp (SW600 Ad300).

P-gp BCRP-IN-2 (compound 15), an oxadiazole derivative, functions as a dual inhibitor targeting both the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). Additionally, it bolsters the anti-proliferative impact of Doxorubicin in the drug-resistant HT29 DX and MDCK-MDR1 human adenocarcinoma colon cancer cell lines [1].

CGP 25454A is a novel and selective antagonist of the presynaptic dopamine autoreceptor (CGP 25454A).

Cgp 29287 is a primate-specific renin inhibitor. It also has a prolonged duration of action.

CGP 28392 is used as a partial calcium channel agonist.

CGP 20309 is a kind of thiocarbonylamide with high anti filamentous activity.

CGP 21833 is an antifilarial agent.

CGP 22979 is a renal selective vasodilator prodrug.

CGP 23996 is a non-reducible somatostatin analog used for autoradiography.

Cgp 28861 reverses the effects of calcium channel blockaders in the frog heart.

AVE5688, an inhibitor of glycogen phosphorylase (GP), has IC50 values of 430 nM and 915 nM, and Kd values of 170 nM and 530 nM for rmGPb and rmGPa, respectively. It is suitable for research on type 2 diabetes.

GP2-114 is a catecholamine motility mimetic that produces current-dependent cardiovascular effects when administered via transdermal iontophoresis and can be used to study coronary artery disease (CAD).

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4 6, exhibiting IC50 values of 1.5 μM for CDK4 cyclin D1, 5.6 μM for CDK6 cyclin D1, and 25 μM for Cdk5 p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1 2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

FM04 is an orally active and highly potent inhibitor of P-glycoprotein (P-gp) with an EC50 value of 83 nM. FM04 can interact with Q1193 and I1115 in human P-gp nucleotide binding domain 2 (NBD2). Thereby disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling the ICL2-NBD2 interaction, thereby inhibiting P-gp. FM04 can be used in the treatment of cancer and tumors.

Diclofenac sodium (GP 45840) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Levofloxacin ((-)-Ofloxacin) is a synthetic fluoroquinolone antibiotic that inhibits the superhelical activity of bacterial DNA rotamase and prevents DNA replication. Levofloxacin is a broad-spectrum antibiotic used for the treatment of a wide range of bacterial infections.

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

R 59-022 (DKGI-I) is a diacylglycerol kinase (DGK) inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells. R 59-022 activates protein kinase C (PKC), inhibits intestinal smooth muscle contractility, and enhances O2- production induced by 1-oleoyl-2-acetylglycerol.

GP-515 HCl is an adenosine kinase inhibitor. In cultured rat myocardial myocytes (RMMs), GP-515 can induce the expression of vascular endothelial growth factor (VEGF). Under severe hypoxia (1% O(2)), GP-515 (20 microM) does not affect VEGF protein expression, but under mild hypoxic conditions, it increases VEGF expression by 27%.