SGC stimulator 2
SGC stimulator 2 is an orally active soluble guanylyl cyclase (sGC) stimulator with an EC50 of 44 nM. SGC stimulator 2 exhibits inhibitory activity against the CB2 receptor, with an IC50 of 2.7 μM. SGC stimulator 2 activates native (Fe2+) sGC in a heme-dependent manner. SGC stimulator 2 produces sustained hypotensive effects in animal models. SGC stimulator 2 can be used for the research of hypertension.
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- CAS No.: 1350852-88-8
- Formule: C24H18ClF5N6O
- Masse moléculaire:536.88
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
SGC stimulator 2 (Compound 20) potently stimulates human sGC α1/β1 in CHO cells with an EC50 of 44 nM via a heme-dependent mechanism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SGC stimulator 2 (Compound 20) (0.1 mg/kg; p.o.; single dose) produces sustained blood pressure lowering in conscious telemetered beagle dogs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:spontaneously hypertensive rats (male)[1]
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Dosage:0.03 mg/kg (chronic); 0.03, 0.1, 0.3 and 1 mg/kg (acute single dose)
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Administration:p.o.; once daily; 15 days (chronic); p.o.; single dose (acute)
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Result:Reduced systolic blood pressure by 85 mmHg at 4 hours after single 1 mg/kg oral dose.
Produced dose-dependent reductions in mean, systolic, diastolic, and pulse pressures, with effects sustained for >24 hours following single oral doses of 0.03-1 mg/kg.
Achieved consistent systolic blood pressure reductions of ~15-20 mmHg with full 24-hour coverage and no tachyphylaxis during once-daily oral administration of 0.03 mg/kg for 15 days.
Diminished modest reflex tachycardia (HR ~40 beats/min) observed on day 1 by days 4-5, and maintained stable plasma exposures (C_max ~2.5 nM; C_trough ~0.5 nM) during chronic dosing.
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Animal Model:beagle dogs (male)[1]
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Dosage:0.1 mg/kg
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Administration:p.o.; single dose
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Result:Reduced systolic blood pressure by 20 mmHg at 6 hours after single 0.1 mg/kg oral dose.
Maintained a sustained ~10 mmHg systolic blood pressure decrease through 36 hours post-dose.
Sustained a maximal ~20 beats/min reflexogenic increase in heart rate out to 36 hours post-dose.
Chemical Information
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CAS No. 1350852-88-8
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Masse moléculaire 536.88
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Formule C24H18ClF5N6O
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SMILES
ClC1=CC2=C(C=C1)C(C3=NC(NC([C@@]4(C)C5=CC=CC=C5)=O)=C4C(N)=N3)=NN2CCC(F)(F)C(F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SGC stimulator 2 Related Classifications
HY-187209 Related Classifications
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