Cat. No.: HY-161834

RG100204

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.50%
CAS No.: 2140901-88-6
Formula: C₂₀H₂₆N₆O₂S₂
Molecular Weight:446.59

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RG100204 Chemical Structure

CAS No.: 2140901-88-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

NLRP3

All NOD-like Receptor (NLR) Isoforms :

All p38 MAPK Isoforms :

In Vitro

RG100204 (25 μM; 6 h) attenuates lipopolysaccharide-induced superoxide anion and NO production in FaO hepatoma cells without affecting cell viability^[1].
RG100204 (50 nM-1 μM; 5-50 min) inhibits AQP9-mediated water and glycerol permeability in CHO cells expressing human AQP9, with IC₅₀ values of approximately 50 nM for both substrates^[2].
RG100204 (25 μM; 10 min) significantly reduces the glycerol permeability coefficient in proteoliposomes containing recombinant human AQP9^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RG100204 (25 mg/kg; po; once before and 8 h after surgery; single dose) alleviates hypothermia, cardiac (systolic/diastolic function) and renal dysfunction, reduces liver damage and inflammatory factor release, and inhibits NLRP3 inflammasome and p38 MAPK signaling pathway activation in a cecal ligation and puncture (CLP)-induced sepsis model in C57BL/6 male mice^[1].
RG100204 (5-50 mg/kg; po; single dose) increases plasma glycerol levels in a dose-dependent manner in a diabetic mouse model, with an insignificant trend toward lowering blood glucose^[2].
RG100204 (25 mg/kg; po; once daily; 28 days) improves body weight loss, colon shortening and ulcers, inhibits the expression of inflammatory factors (TNF-α, IL-6) and pyroptosis-related proteins, and alleviated colon tissue damage in a trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 male mice (20-30 g, 10-week-old) with cecal ligation and puncture (CLP)-induced sepsis model^[1]
Dosage:

25 mg/kg (formulated in PEG 400)
Administration:

Oral gavage, once before CLP and once 8 h after surgery, single dose
Result:

Attenuated hypothermia, improved cardiac systolic (ejection fraction, fractional shortening) and diastolic function (mitral valve E/A ratio), reduced serum creatinine and LDH levels, decreased hepatic injury markers (ALT, AST), and suppressed activation of NLRP3 inflammasome (reduction in NLRP3, cleaved caspase-1) and p38 MAPK signaling (phosphorylated p38 MAPK) in heart and kidney tissues.

Animal Model:

C57BLKS db/db male mice (10-week-old) with diabetic model^[2]
Dosage:

5, 12.5, 25, 50 mg/kg (formulated in Tetraethylene glycol (HY-W018745)
Administration:

Oral gavage, single dose, fasting throughout 6 h observation
Result:

Significantly increased plasma glycerol levels in a dose-dependent manner (e.g., 25 mg/kg and 50 mg/kg groups showed ~30% and ~45% increase vs. control), while resulting a non-significant downward trend in blood glucose in all treated groups compared to vehicle control.

Animal Model:

BALB/c male mice (18-22 g, 8-week-old) with TNBS-induced colitis model^[3]
Dosage:

25 mg/kg
Administration:

Oral gavage, once daily for 28 d
Result:

Reduced disease severity scores (e.g., decreased ulceration and epithelial damage in colon histology), increased colon length, lower levels of serum TNF-α and IL-6, and reduced expression of pyroptosis markers (GSDMD-N, IL-1β, IL-18) and NLRP3 inflammasome components (NLRP3, ASC, cleaved caspase-1) in colon tissues.

Chemical Information

CAS No. 2140901-88-6
Appearance Solid
Molecular Weight 446.59
Formula C₂₀H₂₆N₆O₂S₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Mol Biotechnol

Correction: Downregulation of AQP9 Ameliorates NLRP3 Inflammasome-Dependent Inflammation and Pyroptosis in Crohn's Disease by Inhibiting the p38 MAPK Signaling Pathway. [Abstract]

2026 Mar 14. PMID: 41830972

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (111.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2392 mL

11.1960 mL

22.3919 mL

5 mM

0.4478 mL

2.2392 mL

4.4784 mL

10 mM

0.2239 mL

1.1196 mL

2.2392 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2392 mL	11.1960 mL	22.3919 mL	55.9798 mL
	5 mM	0.4478 mL	2.2392 mL	4.4784 mL	11.1960 mL
	10 mM	0.2239 mL	1.1196 mL	2.2392 mL	5.5980 mL
	15 mM	0.1493 mL	0.7464 mL	1.4928 mL	3.7320 mL
	20 mM	0.1120 mL	0.5598 mL	1.1196 mL	2.7990 mL
	25 mM	0.0896 mL	0.4478 mL	0.8957 mL	2.2392 mL
	30 mM	0.0746 mL	0.3732 mL	0.7464 mL	1.8660 mL
	40 mM	0.0560 mL	0.2799 mL	0.5598 mL	1.3995 mL
	50 mM	0.0448 mL	0.2239 mL	0.4478 mL	1.1196 mL
	60 mM	0.0373 mL	0.1866 mL	0.3732 mL	0.9330 mL
	80 mM	0.0280 mL	0.1399 mL	0.2799 mL	0.6997 mL
	100 mM	0.0224 mL	0.1120 mL	0.2239 mL	0.5598 mL

Keywords

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RG100204

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Membrane Transporter/Ion Channel Compound Library

NF-κB Signaling Compound Library

Antioxidant Compound Library

Reprogramming Compound Library

Anti-diabetic Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Ion Channel Compound Library

Anti-Ovarian Cancer Compound Library

Inflammasomes related Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) RG100204

All NOD-like Receptor (NLR) Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RG100204 Related Classifications

HY-161834 Related Classifications