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RG100204

Chemical Structure : RG100204

CAS No.: 2140901-88-6

RG100204 (RG 100204)

Catalog No.: PC-47092Not For Human Use, Lab Use Only.

RG100204 is a novel selective, small molecule inhibitor of the neutral solute channel Aquaporin 9 (AQP9), inhibits AQP9 water permeability (IC50=110 nM) and AQP9 glycerol permeability (IC50=76 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RG100204 is a novel selective, small molecule inhibitor of the neutral solute channel Aquaporin 9 (AQP9), inhibits AQP9 water permeability (IC50=110 nM) and AQP9 glycerol permeability (IC50=76 nM).
RG100204 displays no inhibition of water or glycerol permeability in AQP3 expressing CHO cells, and only minor inhibition of AQP7.
RG100204 inhibits AQP9 H2O2 permeability with similar potency and efficacy as for water and glycerol permeability.
RG100204 effectively attenuates CLP-induced systolic cardiac dysfunction in septic mice, attenuates CLP-induced hepatocellular injury and renal dysfunction, effectively inhibits the NF-ĸB signalling pathway in the kidney.

Physicochemical Properties

M.Wt 446.588
Formula C20H26N6O2S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[[4-Ethyl-5-(1-methylethyl)-4H-1,2,4-triazol-3-yl]thio]-N-[5-[4-(1-methylethoxy)phenyl]-1,3,4-thiadiazol-2-yl]acetamide

References

1. Mohammad S, et al. Front Immunol. 2022 Jun 14;13:900906.

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