2. Apoptosis Immunology/Inflammation Membrane Transporter/Ion Channel MAPK/ERK Pathway
  3. Pyroptosis Aquaporin NOD-like Receptor (NLR) p38 MAPK
  4. 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.

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RG100204 Chemical Structure

RG100204 Chemical Structure

CAS No. : 2140901-88-6

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Based on 1 publication(s) in Google Scholar

RG100204 Related Antibodies

Top Publications Citing Use of Products

View All NOD-like Receptor (NLR) Isoform Specific Products:

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NLRP3 NLRP1 NOD1 NOD2

View All p38 MAPK Isoform Specific Products:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Description

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].

IC50 & Target

NLRP3

 

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.

RG100204 Related Antibodies
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.
Molecular Weight

446.59

Formula

C20H26N6O2S2
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2392 mL 11.1960 mL 22.3919 mL
5 mM 0.4478 mL 2.2392 mL 4.4784 mL
View the Complete Stock Solution Preparation Table

* 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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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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RG100204 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RG1002042140901-88-6RG 100204RG-100204PyroptosisAquaporinNOD-like Receptor (NLR)p38 MAPKAQPSepsiscardiac dysfunctionrenal dysfunctionCHOFaO hepatoma cellsanti-inflammatory activityInhibitorinhibitorinhibit

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