2. GPCR/G Protein
  3. Guanylate Cyclase
  4. Cinaciguat hydrochloride

Cinaciguat hydrochloride  (Synonyms: BAY 58-2667 hydrochloride)

Cat. No.: HY-14181A Purity: 98.90%
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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.

Cinaciguat hydrochloride Chemical Structure

Cinaciguat hydrochloride Chemical Structure

CAS No. : 646995-35-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 238 In-stock
Solution
10 mM * 1 mL in DMSO USD 238 In-stock
Solid
2 mg USD 120 In-stock
5 mg USD 180 In-stock
10 mg USD 300 In-stock
50 mg USD 620 In-stock
100 mg USD 880 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Cinaciguat hydrochloride:

Cinaciguat hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Cinaciguat hydrochloride is a potent soluble guanylate cyclase (GC) activator with EC50 of 15 nM in platelets.

IC50 & Target

EC50:15 nM (Guanylate cyclase)[1]
In Vitro

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.

Cinaciguat hydrochloride Related Antibodies
In Vivo

Administration of Cinaciguat decreased BP and increased HR in both apo-sGC mice and WT mice. In fact, the BP-lowering effect of Cinaciguat in apo-sGC mice is significantly greater and longer lasting than in WT mice. In addition, Cinaciguat decreased BP in apo-sGC mice at concentrations that did not affect BP in WT mice. Furthermore, the IC50 values for Cinaciguat-induced ex vivorelaxation of precontracted aortas are threefold lower in apo-sGC mice than in WT mice (IC50=0.2 nM and 0.7 nM, respectively). Together, our results suggest that sGC activators like Cinaciguat but not sGC stimulators like BAY 41-2272 activate apo-sGC. In addition, the observation that Cinaciguat can modulate vasorelaxation and BP in WT mice suggests that even in healthy mice, a subset of the available sGC pool is haem-free and responsive to sGC activators[2].

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

602.16

Formula

C36H40ClNO5
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6607 mL 8.3034 mL 16.6069 mL
5 mM 0.3321 mL 1.6607 mL 3.3214 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 (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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.75 mg/mL (4.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

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.

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

Cinaciguat646995-35-9BAY 58-2667Guanylate CyclaseInhibitorinhibitorinhibit

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