2. GPCR/G Protein
  3. Guanylate Cyclase
  4. Runcaciguat

Runcaciguat  (Synonyms: BAY 1101042)

目录号: HY-109136 纯度: 99.31%
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Runcaciguat (BAY 1101042) 是一种选择性、口服有效的可溶性鸟苷酸环化酶 (sGC) 别构激活剂，专门靶向其氧化和无血红素形式。Runcaciguat 以组氨酸依赖的方式结合 sGC，在氧化应激下恢复环磷酸鸟苷 (cGMP) 生成，不依赖一氧化氮 (NO) 或血红素。Runcaciguat 具有肾保护和心脏保护活性，如减少蛋白尿和改善肾功能。Runcaciguat 主要用于研究与高血压、糖尿病和代谢紊乱相关的慢性肾病 (CKD)，以及心力衰竭保留射血分数 (HFpEF) 等潜在心血管适应症。

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Runcaciguat

Runcaciguat Chemical Structure

CAS No. : 1402936-61-1

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1123
In-stock
1 mg ￥430
In-stock
5 mg ￥1045
In-stock
10 mg ￥1550
In-stock
25 mg ￥2510
In-stock
50 mg ￥4395
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Runcaciguat 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Runcaciguat (BAY 1101042) is a selective, orally active, allosteric activator of soluble guanylate cyclase (sGC) that specifically targets its oxidized and heme-free form. Runcaciguat binds to sGC in a histidine-dependent manner and restores cyclic guanosine monophosphate (cGMP) production under oxidative stress, independent of nitric oxide (NO) or heme. Runcaciguat exhibits renoprotective and cardioprotective activities, such as reduced proteinuria and improved renal function. Runcaciguat is primarily being studied in chronic kidney disease (CKD) associated with hypertension, diabetes, and metabolic disorders, as well as potential cardiovascular indications such as heart failure with preserved ejection fraction (HFpEF)[1][2][3].

IC50 & Target

sGC

 

体外研究
(In Vitro)

Runcaciguat (100 pM-10 μM；10 min) 激活 HEK293 细胞中野生型可溶性鸟苷酸环化酶 (sGC，EC50=789 nM)，但对 β1H105A/F 突变体无活性，证实其激活依赖 β1 亚基组氨酸 105 残基[1]。

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

Runcaciguat 相关抗体:
体内研究
(In Vivo)

Runcaciguat (1-10 mg/kg；口服灌胃或混饲；每日 1-2 次；2-12 周) 在 ANG-SD 大鼠、RenTG 大鼠、ZDF 大鼠及 ZSF1 大鼠等慢性肾病 (CKD) 模型中，显著降低蛋白尿、改善肾功能标志物 (如 Cyst-C、KIM-1)、减轻肾脏病理损伤 (如肾小球硬化、肾小管退化)，并提高 RenTG 大鼠的生存率[2][3]。

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

Animal Model: Sprague-Dawley (SD) rats (male, ~260 g, 12 weeks) with ANG II-induced hypertensive nephropathy model[2]
Dosage: 0.3, 1, 3 mg/kg
Administration: Oral gavage, bid, 2 weeks
Result: Reduced proteinuria (uPCR) by 30%-50% compared to vehicle, decreased renal injury markers (NGAL, KIM-1, OPN gene expression), and improved creatinine clearance without significant blood pressure reduction.
Animal Model: RenTG rats (male, 8 weeks) with L-NAME-supplemented hypertensive CKD model[2]
Dosage: 3, 10 mg/kg
Administration: Oral gavage, bid, 8 weeks
Result: Increased survival rate (from 42% to 61%-72%), reduced left ventricular hypertrophy (LVW/BW ratio ↓14%-17%), and decreased proteinuria (uPCR ↓54%-70%) with improved creatinine clearance.
Animal Model: ZDF rats (male, 22 weeks) with diabetic CKD model[2]
Dosage: 140 ppm (equivalent to 3 mg/kg bid; mixed in food)
Administration: Dietary admixture, daily, 42 weeks
Result: Reduced proteinuria (uPCR ↓54% at 3 mg/kg equivalent), improved renal histopathology (tubular degeneration and glomerulopathy grades ↓1-2), and decreased plasma markers of injury (OPN, cystatin C). HbA1c, triglycerides, and cholesterol were also reduced by 8%-76%, suggesting metabolic benefits.
Clinical Trial
分子量

488.33

Formula

C23H22Cl2F3NO3
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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (255.97 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 2.0478 mL 10.2390 mL 20.4780 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 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 (protect from light)。-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

Runcaciguat 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 (protect from light)。-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 2.0478 mL 10.2390 mL 20.4780 mL 51.1949 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 mL 10.2390 mL
10 mM 0.2048 mL 1.0239 mL 2.0478 mL 5.1195 mL
15 mM 0.1365 mL 0.6826 mL 1.3652 mL 3.4130 mL
20 mM 0.1024 mL 0.5119 mL 1.0239 mL 2.5597 mL
25 mM 0.0819 mL 0.4096 mL 0.8191 mL 2.0478 mL
30 mM 0.0683 mL 0.3413 mL 0.6826 mL 1.7065 mL
40 mM 0.0512 mL 0.2560 mL 0.5119 mL 1.2799 mL
50 mM 0.0410 mL 0.2048 mL 0.4096 mL 1.0239 mL
60 mM 0.0341 mL 0.1706 mL 0.3413 mL 0.8532 mL
80 mM 0.0256 mL 0.1280 mL 0.2560 mL 0.6399 mL
100 mM 0.0205 mL 0.1024 mL 0.2048 mL 0.5119 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:

Runcaciguat1402936-61-1BAY 1101042BAY1101042BAY-1101042Guanylate CyclaseInhibitorinhibitorinhibit

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