2. Apoptosis Immunology/Inflammation Membrane Transporter/Ion Channel MAPK/ERK Pathway
  3. Pyroptosis Aquaporin NOD-like Receptor (NLR) p38 MAPK
  4. RG100204

RG100204 是一种选择性、口服有效的水通道蛋白 AQP9 的抑制剂。RG100204 可直接抑制 AQP9 通道功能，阻止水、甘油及 H2O2 的跨膜运输。RG100204 可减少 NLRP3 炎症小体和 p38 MAPK 信号通路的激活，从而减轻炎症和焦亡。RG100204 在小鼠脓毒症模型中可减轻多器官功能障碍，并在糖尿病 db/db 小鼠中显示调节血糖的作用。

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RG100204 Chemical Structure

RG100204 Chemical Structure

CAS No. : 2140901-88-6

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5 mg ￥1610
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10 mg ￥2590
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25 mg ￥5460
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Customer Review

RG100204 相关抗体

Top Publications Citing Use of Products

查看 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

RG100204 (25 μM；6 h) 在 FaO 肝癌细胞实验中减弱脂多糖诱导的超氧阴离子和 NO 产生，且不影响细胞活力[1]。
RG100204 (50 nM-1 μM；5-50 min) 在表达人 AQP9 的 CHO 细胞中抑制 AQP9 介导的水和甘油通透性，对两种底物的 IC50 值均约为 50 nM[2]。
RG100204 (25 μM；10 min) 在重组人 AQP9 的蛋白脂质体实验中显著降低甘油通透系数[2]。

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

RG100204 相关抗体:
体内研究
(In Vivo)

RG100204 (25 mg/kg；口服；术前及术后 8 h 各 1 次；单次) 在C57BL/6雄性小鼠 (20-30 g，10周龄) 盲肠结扎穿刺 (CLP) 诱导的脓毒症模型中，减轻体温降低、心脏 (收缩/舒张功能) 和肾脏功能障碍，减少肝脏损伤及炎症因子释放，并抑制 NLRP3 炎症小体和 p38 MAPK 信号通路激活[1]。
RG100204 (5-50 mg/kg；口服；单剂量) 在糖尿病小鼠模型中，呈剂量依赖性升高血浆甘油水平，血糖降低趋势但未达统计学显著[2]。
RG100204 (25 mg/kg；口服；每日 1 次；28 d) 在三硝基苯磺酸 (TNBS) 诱导的小鼠结肠炎模型中，改善体重下降、结肠缩短及溃疡，抑制炎症因子 (TNF-α、IL-6) 和焦亡相关蛋白表达，减轻结肠组织损伤[3]。

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.
分子量

446.59

Formula

C20H26N6O2S2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (111.96 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

RG100204 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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