Cinaciguat hydrochloride
Based on 4 publication(s) in Google Scholar
Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.
For research use only. We do not sell to patients.
- Purity: 98.90%
- CAS No.: 646995-35-9
- Formula: C36H40ClNO5
- Molecular Weight:602.16
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Cinaciguat hydrochloride
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Biological Activity
EC50:15 nM (Guanylate cyclase)[1]
In platelets, Cinaciguat (BAY 58-2667) is a potent GC activator (EC50 15 nM) but the maximum effect is only about 1% of that achievable with NO. Concentration-response curves for Cinaciguat are constructed after 1 min exposure in the presence of sildenafil. Without ODQ, the EC50 is 18 nM, and in the presence of ODQ the potency of Cinaciguat is not significantly different, the EC50 being 13 nM. The potency of Cinaciguat in platelets (EC50 15 nM) is very similar to estimates made on purified recombinant GC. Cinaciguat at a maximally effective concentration of 1 μM stimulates control GC activity to about 25% of that observed with NO and, contrasting with the stimulation by NO, this level of activity remained constant as the proportion of ODQ-pretreated GC is increased[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 646995-35-9
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Appearance Solid
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Molecular Weight 602.16
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Formula C36H40ClNO5
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Color White to off-white
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SMILES
OC(C(C=C1)=CC=C1CN(CCCCC(O)=O)CCC(C=CC=C2)=C2OCC(C=C3)=CC=C3CCC4=CC=CC=C4)=O.[H]Cl
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Synonyms
BAY 58-2667 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Differential modulation of the sGC-cGMP pathway by sGC stimulators and activators in human lung cells. [Abstract]2026 Mar 5:248:117866. PMID: 41794266 -
Oxid Med Cell Longev
Pharmic Activation of PKG2 Alleviates Diabetes-Induced Osteoblast Dysfunction by Suppressing PLC β 1-Ca2+-Mediated Endoplasmic Reticulum Stress. [Abstract]2021 Jun 16:2021:5552530. PMID: 34221234 -
Biomed Pharmacother
Cinaciguat in combination with insulin induces a favorable effect on implant osseointegration in type 2 diabetic rats. [Abstract]2019 Oct:118:109216. PMID: 31319371 -
Solvent & Solubility
DMSO : 110 mg/mL (182.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Aliquots of the platelet suspension are withdrawn before and at various times after addition of spermine NONOate or Cinaciguat and transferred immediately into inactivation buffer (50 mM Tris, 4 mM EDTA, pH 7.4) at 100°C for at least 10 min. When used, 10 μM ODQ is added to the platelets 15 min before addition of spermine NONOate. Purified GC activity is measured at a final concentration of 50 ng/mL in assay buffer (50 mM Tris, 100 μM EDTA, 1 mM NaGTP, 1.3 mM MgCl2, 50 μg/mL BSA, pH 7.4), stimulated with DEA/NO (10 μM) or Cinaciguat (1 μM), enzyme inactivation being performed as with platelets. The levels of cGMP are measured by radioimmunoassay and expressed relative to the amount of protein. Three independent runs are carried out in each experiment and the resulting data presented as means±s.e.mean[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Male and female mice (12 weeks old) are anaesthetized with isoflurane, 0.5 cm of the tail tip is removed with a sharp razor blade, and the tail tip is immediately put into fresh pre-warmed PBS of 37°C. The latency until the tail stopped bleeding is visually scored and recorded with a chronometer by an observer blinded to the genotype. Systolic BP (SBP) and heart rate (HR) are measured non-invasively in awake mice by tail-cuff using a Hatteras MC4000 Blood Pressure Analysis System. Mice are habituated to the BP measurement device for 7 days. To determine basal BP, mice are measured for 15 consecutive cycles per day during 5 days. L-NAME (100 mg/kg), SNP (1.5 mg/kg), DETA-NO (60 mg/kg), BAY 41-2772 (4 mg/kg), Cinaciguat (30 μg/kg) and the vehicle controls (PBS or for the BAY-compounds 20% Cremophor+20% diethylene-glycol-monoethyl-ether in PBS) are all administered IP. After SNP administration, SBP measurements are recorded from 5 to 15 min post injection, for L-NAME and DETA-NO recordings are made from 1 to 25 min post injection and for BAY-compounds recordings are made from 10 to 25 min post injection.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Roy B, et al. Probing the presence of the ligand-binding haem in cellular nitric oxide receptors. Br J Pharmacol. 2008 Apr;153(7):1495-504. [Content Brief]
[2]. Thoonen R, et al. Cardiovascular and pharmacological implications of haem-deficient NO-unresponsive soluble guanylate cyclase knock-in mice. Nat Commun. 2015 Oct 7;6:8482. [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 (sealed storage, away from moisture). 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 | 1.6607 mL | 8.3034 mL | 16.6069 mL | 41.5172 mL |
| 5 mM | 0.3321 mL | 1.6607 mL | 3.3214 mL | 8.3034 mL | |
| 10 mM | 0.1661 mL | 0.8303 mL | 1.6607 mL | 4.1517 mL | |
| 15 mM | 0.1107 mL | 0.5536 mL | 1.1071 mL | 2.7678 mL | |
| 20 mM | 0.0830 mL | 0.4152 mL | 0.8303 mL | 2.0759 mL | |
| 25 mM | 0.0664 mL | 0.3321 mL | 0.6643 mL | 1.6607 mL | |
| 30 mM | 0.0554 mL | 0.2768 mL | 0.5536 mL | 1.3839 mL | |
| 40 mM | 0.0415 mL | 0.2076 mL | 0.4152 mL | 1.0379 mL | |
| 50 mM | 0.0332 mL | 0.1661 mL | 0.3321 mL | 0.8303 mL | |
| 60 mM | 0.0277 mL | 0.1384 mL | 0.2768 mL | 0.6920 mL | |
| 80 mM | 0.0208 mL | 0.1038 mL | 0.2076 mL | 0.5190 mL | |
| 100 mM | 0.0166 mL | 0.0830 mL | 0.1661 mL | 0.4152 mL |
Cinaciguat hydrochloride Related Classifications
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