Drug intelligence / Profile preview

GYY4137

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

GYY4137 is a water-soluble, small molecule hydrogen sulfide (H2S) donor that releases H2S slowly over time. It is primarily used in preclinical research as a tool compound to study the biological effects of sustained H2S release. Mechanistically, GYY4137 acts as an H2S donor, exerting anti-inflammatory, cardioprotective, vasodilatory, antihypertensive, and neuroprotective effects in various animal models. Its actions are mediated through modulation of signaling pathways such as NF-κB and MAPK (including p38, ERK1/2, JNK1/2), inhibition of pro-inflammatory cytokine production (e.g., TNF-α, IL-1β, IL-6), reduction of oxidative stress markers (e.g., malondialdehyde), enhancement of antioxidant enzymes (e.g., SOD and Nrf2), and improvement in endothelial function. Preclinical studies have shown efficacy in models of cardiovascular disease (hypertension and myocardial infarction), osteoarthritis, peritoneal fibrosis, chronic intestinal barrier injury/obesity-related gut dysfunctions, Parkinson’s disease models via neuroprotection against dopaminergic neuron degeneration and α-synuclein nitration reduction[1][2][3][4][5][6][7][8][9].

Other names
vasodilators(NUS)
02

Targets

H2S (Hydrogen sulfide)

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