Activators & Inhibitors

AMPA-IN-1 is a potent inhibitor of AMPA receptors, a widely expressed receptor in the brain with a central role in the regulation of rapid excitatory synaptic transmission and synaptic plasticity. 14).

AMG8788 is a selective, potent and orally active TRPM8 antagonist (IC50: 63.2 nM).

HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1. HIV-1 inhibitor-16 also showed some inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM, respectively. HIV-1 inhibitor-16 showed good solubility and hepatic microsomal stability and did not exhibit significant CYP enzyme inhibitory activity or acute toxicity.

IDO-IN-16 (compound 5) is an IDO inhibitor (IC50: 36 nM).

α-Synuclein inhibitor 5 is a potent inhibitor of α-Synuclein (α-Syn) aggregation across the blood-brain barrier (IC50: 1.22 μM), with 94.3% inhibition at 30 μM.

S-777469 is a selective, orally active agonist of the cannabinoid type 2 receptor (CB2) (Ki: 36 nM). s-777469 significantly inhibited compound 48/80-induced scratching behaviour in mice in a dose-dependent manner. s-777469 excites CB2, inhibits pruritic signalling and shows an anti-pruritic effect.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator (IC50<1 nM) that can be used to study neuropsychiatric disorders.

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

Tubulin polymerization-IN-25 is a selective, dual tubulin polymerization (IC50: 1.11 μM) and farnesyl transferase (FTase) (IC50: 0.39 μM) inhibitor. polymerization-IN-25 exhibits cytotoxicity against cancer cells and blocks cell proliferation.