製品番号: HY-161834

RG100204

1 Cited Publications

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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.50%
CAS 番号: 2140901-88-6
分子式: C₂₀H₂₆N₆O₂S₂
分子量:446.59

保管条件:

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

RG100204 構造式

CAS 番号: 2140901-88-6

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Amount: USD 0.00

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Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

NLRP3

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示 :

p38 MAPK アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2140901-88-6
性状 Solid
分子量 446.59
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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

View the Complete Stock Solution Preparation Table

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

RG100204

1 Cited Publications

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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

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Anti-Prostate Cancer Compound Library

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Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

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Anti-Ovarian Cancer Compound Library

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MCE Bioactive Compound Library

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High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Lactylation Compound Library

MedChemExpress（MCE）の使用を引用している文献 RG100204

NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示

p38 MAPK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

RG100204 関連分類

HY-161834 関連分類