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

Runcaciguat  (Synonyms: BAY 1101042)

Cat. No.: HY-109136 Purity: 99.31%
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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).

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Runcaciguat Chemical Structure

Runcaciguat Chemical Structure

CAS No. : 1402936-61-1

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Runcaciguat Related Antibodies

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Description

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

 

In Vitro

Runcaciguat (100 pM-10 μM; 10 min) activates wild-type soluble guanylate cyclase (sGC, EC50=789 nM) in HEK293 cells, but inactive against the β1H105A/F mutant, confirming that its activation is dependent on the histidine 105 residue of the β1 subunit[1].

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

Runcaciguat Related Antibodies
In Vivo

Runcaciguat (1-10 mg/kg; oral gavage or mixed feed; 1-2 times a day; 2-12 weeks) significantly reduces proteinuria, improves renal function markers (such as Cyst-C, KIM-1), alleviates renal pathological damage (such as glomerular sclerosis, tubular degeneration) in chronic kidney disease (CKD) models such as ANG-SD rats, RenTG rats, ZDF rats and ZSF1 rats, and improves the survival rate of RenTG rats[2][3].

MedChemExpress (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
Molecular Weight

488.33

Formula

C23H22Cl2F3NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC([C@H](C2CC2)CC(O)=O)=CC=C1Cl)[C@@](C3=CC=C(Cl)C=C3)([H])[C@@H](C)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (255.97 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 2.0478 mL 10.2390 mL 20.4780 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 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 (protect from light). 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (protect from light). 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 2.0478 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
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Runcaciguat 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:

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

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