1. GPCR/G Protein
  2. Guanylate Cyclase

Cinaciguat (Synonyms: BAY 58-2667)

Cat. No.: HY-14181 Purity: 99.64%
Data Sheet SDS Handling Instructions

Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.

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Cinaciguat Chemical Structure

Cinaciguat Chemical Structure

CAS No. : 329773-35-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $187 In-stock
2 mg $100 In-stock
5 mg $150 In-stock
10 mg $250 In-stock
50 mg $900 In-stock
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  • Technical Information

  • Purity & Documentation

  • References

Description

Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure.

In Vitro

Cinaciguat (10 μM) significantly enhances intracellular cGMP generation. Cinaciguat does not dose-dependent effects on cell contraction and calcium transients[2].

In Vivo

Cinaciguat (10 mg/kg/day, p.o.) treatment in diabetic rats does not influence blood glucose levels, but leads to attenuated water intake. Cinaciguat treatment alleviates diabetes mellitus related oxidative stress, protects against DM related alteration of the NO-sGC-cGMP-PKG signalling, and alleviates DM related myocardium hypertrophy and apoptosis[1]. Cinaciguat (1-10-100 nM) induces concentration-dependent relaxations in strips from both WT and apo-sGC mice, but does not have any effect on phasic activity induced by PGF in WT or apo-sGC strips[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00559650 Bayer Congestive Heart Failure December 2007 Phase 2
NCT01067859 Bayer Acute Heart Failure March 2010 Phase 2
NCT01064037 Bayer Heart Failure|Heart Decompensation April 2010 Phase 2
NCT01065077 Bayer Acute Heart Failure March 2010 Phase 2
NCT00559650 Bayer Congestive Heart Failure December 2007 Phase 2
NCT01067859 Bayer Acute Heart Failure March 2010 Phase 2
NCT01064037 Bayer Heart Failure|Heart Decompensation April 2010 Phase 2
NCT01065077 Bayer Acute Heart Failure March 2010 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.7677 mL 8.8386 mL 17.6772 mL
5 mM 0.3535 mL 1.7677 mL 3.5354 mL
10 mM 0.1768 mL 0.8839 mL 1.7677 mL
Animal Administration
[1]

Cinaciguat is suspended in 0.5 % methylcellulose solution.

After confirmation of DM, rats are randomised into four groups: vehicle-treated control, cinaciguat-treated control, vehicle-treated diabetic and cinaciguat-treated diabetic groups. Animals are treated for 8 weeks with 0.5% methylcellulose vehicle or with the sGC activator cinaciguat in suspension p.o. (10 mg/kg/day), starting immeadiately after DM confirmation. Water bottles are filled every morning with the same amount of fresh tap water and daily water intake is measured. Animal cages are handled with care and are not moved after water bottle replacement to prevent spilling of water from the bottles. Body weight of the animals are recorded every 2 days and the dose of cinaciguat is adjusted accordingly. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

565.7

Formula

C₃₆H₃₉NO₅

CAS No.

329773-35-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Cinaciguat
Cat. No.:
HY-14181
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