Runcaciguat
Based on 1 publication(s) in Google Scholar
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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- Pureza: 99.31%
- No. CAS: 1402936-61-1
- Fòrmula: C23H22Cl2F3NO3
- Peso molecular:488.33
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Runcaciguat
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Actividad biológica
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sGC |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (male, ~260 g, 12 weeks) with ANG II-induced hypertensive nephropathy model[2]
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Dosage:0.3, 1, 3 mg/kg
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Administration:Oral gavage, bid, 2 weeks
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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.
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Animal Model:RenTG rats (male, 8 weeks) with L-NAME-supplemented hypertensive CKD model[2]
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Dosage:3, 10 mg/kg
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Administration:Oral gavage, bid, 8 weeks
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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.
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Animal Model:ZDF rats (male, 22 weeks) with diabetic CKD model[2]
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Dosage:140 ppm (equivalent to 3 mg/kg bid; mixed in food)
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Administration:Dietary admixture, daily, 42 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1402936-61-1
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Appearance Solid
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Peso molecular 488.33
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Fòrmula C23H22Cl2F3NO3
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Color White to off-white
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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
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Synonyms
BAY 1101042
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wittrien T, et al. Runcaciguat activates soluble guanylyl cyclase via the histidine essential for heme binding and nitric oxide activation. Biochem Pharmacol. 2025 Feb;232:116739. [Content Brief]
[2]. Bénardeau A, et al. Runcaciguat, a novel soluble guanylate cyclase activator, shows renoprotection in hypertensive, diabetic, and metabolic preclinical models of chronic kidney disease. Naunyn Schmiedebergs Arch Pharmacol. 2021 Dec;394(12):2363-2379. [Content Brief]
[3]. Kraehling JR, et al. The sGC Activator Runcaciguat Has Kidney Protective Effects and Prevents a Decline of Kidney Function in ZSF1 Rats. Int J Mol Sci. 2023 Aug 25;24(17):13226. [Content Brief]
[4]. Duh EJ, et al. Neuroprotective Effect of a Novel Soluble Guanylate Cyclase Activator (sGCa) Runcaciguat in Diabetes and Ischemic Retinopathy. Diabetes. 2025 Apr 18:db240739. [Content Brief]
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 |
Runcaciguat Related Classifications
HY-109136 Related Classifications
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