2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Endothelin-Converting Enzyme (ECE) Endothelin Receptor
  4. SM19712 free acid

SM19712 free acid is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 free acid inhibits conversion of big ET-1 to ET-1. SM19712 free acid attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 free acid can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury.

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SM19712 free acid

SM19712 free acid Chemical Structure

CAS No. : 194542-49-9

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SM19712 free acid Related Antibodies

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Description

SM19712 free acid is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 free acid inhibits conversion of big ET-1 to ET-1. SM19712 free acid attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 free acid can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury[1][2][3][4][5].

In Vitro

SM19712 free acid potently inhibits ECE solubilized from rat lung microsomes with an IC50 of 42 nM[3].
SM19712 (10-300 μM) free acid shows high specificity for ECE, with no significant inhibitory activity against NEP, ACE, 13 tested receptors, or 9 tested enzymes at concentrations up to 300 μM[3].
SM19712 (1-100 μM; 6 h) free acid concentration-dependently inhibits endogenous ET-1 production in cultured porcine aortic endothelial cells with an IC50 of 31 μM[3].
SM19712 (100 μM) free acid exhibits high selectivity for endothelin-converting enzyme, with minimal inhibitory effects on neutral endopeptidase, angiotensin converting enzyme, collagenase IV, and other proteinase classes[4].

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

SM19712 free acid Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ T1/2 CL Bioavailability
Rat[3] 10 mg/kg i.v. 23 μg·h/mL 0.27 h 0.16 L/h/kg /
Rat[3] 10 mg/kg p.o. 1.8 μg·h/mL / / 8.1 %
Rat[3] 30 mg/kg i.v. 75 μg·h/mL 0.27 h 0.42 L/h/kg /
Rat[3] 30 mg/kg p.o. 6.5 μg·h/mL / / 8.1 %
In Vivo

SM19712 (15 mg/kg; p.o.; daily; 5-6 days) free acid partially attenuates Dextran Sodium Sulfate (HY-116282C)-induced colitis in mice[1].
SM19712 (3-30 mg/kg; i.v.; single bolus 5 minutes before occlusion) dose-dependently attenuates ischemia/reperfusion-induced acute renal failure in Sprague-Dawley rats[2].
SM19712 (0.3-30 mg/kg; i.v.; single dose) free acid dose-dependently suppresses Big ET-1-induced pressor responses in rats[3].
SM19712 (10-30 mg/kg; p.o.; single dose) free acid significantly suppresses big ET-1-induced pressor responses in rats by 37.2%[3].
SM19712 (25.9 mg/kg bolus, 1.7 mg/kg/min infusion; i.v.; single bolus followed by continuous infusion; duration of experiment) free acid significantly reduces infarct size, serum ET-1 elevation, and serum CPK activity in a rabbit model of acute myocardial infarction induced by coronary occlusion and reperfusion[3].

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

Animal Model: C57BL/6 mice (~28 g; inflammatory bowel disease induced by 5% 40 kD Dextran Sodium Sulfate (DDS) in drinking water for 5-6 days)[1]
Dosage: 15 mg/kg/day
Administration: p.o.; daily; 5-6 days
Result: Attenuated DSS-induced increases in colonic ET-1 immunostaining.
Reduced DSS-induced PECAM-1 immunostaining.
Attenuated DSS-induced histologic injury and inflammation.
Decreased the incidence of loose stools and fecal blood.
Reduced DSS-induced weight loss.
Significantly decreased the overall disease activity index in DSS-treated mice.
Did not significantly affect DSS-induced colon shortening or tissue myeloperoxidase activity.
Animal Model: Sprague-Dawley rats (male, 10 weeks old, 280-300 g, acute renal failure induced by right nephrectomy 2 weeks prior followed by 45-minute left renal artery and vein occlusion then reperfusion)[2]
Dosage: 3; 10; 30 mg/kg
Administration: i.v.; single bolus 5 minutes before occlusion
Result: Reduced BUN, increased creatinine clearance, reduced urine flow, increased urinary osmolality, and reduced fractional excretion of sodium.
Attenuated tubular necrosis grade, proteinaceous casts grade, and medullary congestion grade.
Reduced renal ET-1 content.
Animal Model: Sprague-Dawley rats (male, 300-400 g, anesthetized, ganglionic-blocked, challenged with Big Edothelin-1)[3]
Dosage: 0.3; 1; 3; 10; 30 mg/kg
Administration: i.v.; single dose
Result: Dose-dependently suppressed the pressor response induced by Big ET-1.
Significantly reduced the pressor response.
Had no effect on baseline pressure or the pressor response induced by mature ET-1.
Animal Model: Sprague-Dawley rats (male, 280-400 g, conscious then anesthetized, challenged with big endothelin-1)[3]
Dosage: 10; 30 mg/kg
Administration: p.o.; single dose
Result: Produced a 37.2% suppression of the big ET-1-induced pressor response at 30 mg/kg.
Animal Model: New Zealand White rabbits (male, 2.6-3.5 kg, subjected to 30 minutes of coronary artery occlusion followed by 5 hours of reperfusion)[3]
Dosage: 25.9 mg/kg (bolus); 1.7 mg/kg/min (continuous infusion)
Administration: i.v.; single bolus followed by continuous infusion; duration of experiment
Result: Significantly reduced myocardial infarct size, expressed as a percentage of both the left ventricle area and the area at risk, compared to vehicle.
Significantly attenuated the increase in serum ET-1 concentration and serum CPK activity seen in vehicle-treated rabbits during reperfusion.
Molecular Weight

415.85

Formula

C18H14ClN5O3S
CAS No.
SMILES

O=S(C1=CC=C(C=C1)Cl)(NC(NC2=C(C(C)=NN2C3=CC=CC=C3)C#N)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SM19712 free acid Related Classifications

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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:

SM19712194542-49-9SM 19712SM-19712Endothelin-Converting Enzyme (ECE)Endothelin ReceptorEndothelin-Converting EnzymeECEendothelin converting enzymeischemic acute renal failurerat lung microsomesinflammatory bowel diseaseacute myocardial infarctionhuman middle meningeal arteriesSprague-Dawley ratsporcine aortic endothelial cellshuman coronary arteriesC57BL/6 miceInhibitorinhibitorinhibit

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