Mosliciguat
Mosliciguat (BAY 1237592) is an apo-soluble guanylate cyclase activator. Mosliciguat improves cardiopulmonary circulation, reduces pulmonary arterial pressure in animal models, and its efficacy is enhanced under oxidative stress conditions. Mosliciguat exerts a bronchodilatory effect in a rat model of acetylcholine-induced bronchoconstriction. Mosliciguat can be used for research on pulmonary arterial hypertension.
For research use only. We do not sell to patients.
- CAS No.: 2231749-54-3
- Formula: C41H36ClF3N2O5
- Molecular Weight:729.18
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Mosliciguat (0.01-100 μM) potently activates both heme-containing and heme-free (apo) recombinant soluble guanylyl cyclase (sGC) in vitro. Its activity is enhanced in the presence of the sGC inhibitor ODQ (HY-101255), and its action is independent of nitric oxide[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Inhalation administration of Mosliciguat (100 µg/kg via nebulizer) produces a long-lasting (up to 17 hours) inhibitory effect on hypoxia-induced pulmonary hypertension in conscious dogs without affecting heart rate[1].
Mosliciguat (100 µg/kg; administered via inhalation; nebulized, 7 min per dose; 30-100 µg/kg; administered intravenously; cumulative bolus injection) effectively reduces pulmonary arterial pressure in a porcine model of unilateral bronchial obstruction without exacerbating ventilation-perfusion mismatch. In contrast, intravenous administration alone exacerbates desaturation and reduces systemic blood pressure[1].
Mosliciguat (1-100 µg/kg; administered via an aerosol microfeeding system) exerts a dose-dependent bronchodilatory effect in a rat model of acetylcholine-induced bronchoconstriction, with an inhibition rate of pulmonary resistance reaching 68% at the dose of 100 µg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ellegaard Göttinger (female, 4-5 kg body weight, pulmonary hypertension induced by thromboxane A2 analog [U-46619] infusion)[1]
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Dosage:3 µg/kg, 10 µg/kg, 30 µg/kg, 100 µg/kg, 300 µg/kg (inhaled); 1 µg/kg, 3 µg/kg, 10 µg/kg, 30 µg/kg, 100 µg/kg (intravenous)
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Administration:inhaled; via nebulizer, 7 min/dose, cumulative doses; intravenous; cumulative infusions
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Result:Induced a dose-dependent decrease in mean pulmonary arterial pressure (PAP) starting at 10 µg/kg, with no relevant effects on systemic mean blood pressure (BP).
Caused a >5% reduction in PAP versus vehicle at 3 µg/kg.
Achieved maximal PAP reduction 90-120 min after inhalation, maintained for 4 hours.
Did not reduce BP at inhaled 300 µg/kg, while intravenous 30 µg/kg reduced both BP and PAP.
Caused similar or greater PAP reduction than systemic endothelin receptor antagonist or phosphodiesterase type 5 inhibitor at inhaled 30 µg/kg and 100 µg/kg, without reducing BP.
Maintained PAP-lowering efficacy without additional BP effects when combined with endothelin receptor antagonist or phosphodiesterase type 5 inhibitor at inhaled 30 µg/kg.
Showed enhanced PAP reduction without BP effects under oxidative stress (ODQ or L-NAME pretreatment) at inhaled 30 µg/kg.
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Animal Model:Beagle (male, 8-15 kg body weight, pulmonary hypertension induced by hypoxia exposure)[1]
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Dosage:100 µg/kg
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Administration:inhaled; via nebulizer
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Result:Attenuated hypoxia-induced systolic pulmonary arterial pressure (sPAP) increases for 1-17 hours after administration; the effect dissipated by 24 hours.
Caused no effects on heart rate.
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Animal Model:Ellegaard Göttinger (female, 4-5 kg body weight, ventilation/perfusion mismatch induced by unilateral broncho-occlusion)[1]
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Dosage:100 µg/kg (inhaled); 30 µg/kg, 100 µg/kg (intravenous)
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Administration:inhaled; via nebulizer, 7 min/dose; intravenous; cumulative bolus
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Result:Decreased mean pulmonary arterial pressure (PAP) during unilateral ventilation cycles at inhaled 100 µg/kg, with a trend toward reduced desaturation area (no ventilation/perfusion mismatch deterioration) and no effects on systemic BP.
Decreased PAP but increased desaturation area and reduced systemic BP at intravenous 30 µg/kg and 100 µg/kg.
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Animal Model:Brown Norway (male, 10-12 weeks old, bronchoconstriction induced by acetylcholine aerosol provocation)[1]
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Dosage:1 µg/kg, 10 µg/kg, 100 µg/kg
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Administration:inhaled; via aerosolized micro feeding system
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Result:Induced a dose-dependent bronchodilatory effect, inhibiting acetylcholine-induced bronchoconstriction.
Achieved 68% inhibition of lung resistance increase and 37% improvement in dynamic compliance at 100 µg/kg, affecting both large and small airways.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2231749-54-3
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Molecular Weight 729.18
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Formula C41H36ClF3N2O5
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SMILES
OC(C1=CC=C(C2=N1)[C@H](CCC2)N(CCC(C=C3)=CC=C3C(O)=O)CCC(C=CC=C4)=C4OCC(C=CC(C(C=C5)=CC=C5C(F)(F)F)=C6)=C6Cl)=O
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Synonyms
BAY 1237592
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mosliciguat Related Classifications
HY-137446 Related Classifications
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Keywords
- Mosliciguat
- 2231749-54-3
- BAY 1237592
- BAY1237592
- BAY-1237592
- Guanylate Cyclase
- conscious dogs
- nitric oxide
- pulmonary hypertension
- recombinant sGC
- pulmonary vasodilator
- acetylcholine-induced bronchoconstriction rat model
- lung resistance
- ODQ
- apo-soluble guanylate cyclase
- unilateral broncho-occlusion model
- Inhibitor
- inhibitor
- inhibit