RG100204

RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H2O2. RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice[1][2][3].

Product Specifications

CAS Number

[2140901-88-6]

UNSPSC

12352005

Target

Aquaporin; NOD-like Receptor (NLR) ; p38 MAPK; Pyroptosis

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Infection; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/rg100204.html

Purity

99.50

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC(C)OC1=CC=C(C2=NN=C(NC(CSC3=NN=C(C(C)C)N3CC)=O)S2)C=C1

Molecular Formula

C20H26N6O2S2

Molecular Weight

446.59

References & Citations

[1]Mohammad S, et al. RG100204, A Novel Aquaporin-9 Inhibitor, Reduces Septic Cardiomyopathy and Multiple Organ Failure in Murine Sepsis. Front Immunol. 2022 Jun 14;13:900906.|[2]Florio M, et al. Characterization of the Aquaporin-9 Inhibitor RG100204 In Vitro and in db/db Mice. Cells. 2022 Oct 4;11 (19) :3118.|[3]Zhu QQ, et al. Downregulation of AQP9 Ameliorates NLRP3 Inflammasome-Dependent Inflammation and Pyroptosis in Crohn's Disease by Inhibiting the p38 MAPK Signaling Pathway. Mol Biotechnol. 2025 Feb 10.