Sampatrilat - 99%, high purity , CAS No.129981-36-8

  • ≥99%
Item Number
S646677
Grouped product items
SKUSizeAvailabilityPrice Qty
S646677-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$340.90
S646677-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,018.90

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsSampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase ( NEP ). Sampatrilat inhibits C-domain ACE ( K i =13.8 nM) 12.4-fold more potent than that for the N-domain ( K i =171.9 nM). Sampatrilat (UK-812
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
Product Description

Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase ( NEP ). Sampatrilat inhibits C-domain ACE ( K i =13.8 nM) 12.4-fold more potent than that for the N-domain ( K i =171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation

In Vivo

Sampatrilat (oral adminstration; 30 mg/kg; once a day; 5 weeks) reduces the mortality of the rats with CAL (20% versus 57% for untreated\nrats) and increase in the survival rate and improvement of hemodynamic function of the rats with CAL. This compound suppresses tissue ACE and neutral endopeptidase (NEP) activities, but it does not affect the arterial blood pressure, whereas it attenuates the CAL-induced increases in the left ventricular end-diastolic pressure, heart weight, and collagen content of the viable left Ventricle. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Left coronary artery ligation (CAL) and sham-operated ratsDosage: 30 mg/kg Administration: Oral adminstration Result: Prevented the increases in heart weight and cardiac collagen content of the rats with CAL.

Form:Solid

IC50& Target:Ki: 13.8 nM (cACE),171.9 nM (nACE)

Associated Targets(Human)

MME Tclin Neprilysin (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACE Tclin Angiotensin-converting enzyme (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NPPA Tchem Natriuretic peptides A (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACE Tclin Angiotensin-converting enzyme (1423 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MME Tclin Neprilysin (838 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ECE1 Tchem Endothelin-converting enzyme 1 (674 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Canonical SMILES CS(=O)(=O)N[C@@H](CCCCN)C(=O)NC[C@H](CC1(CCCC1)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)O)C(=O)O
Isomeric SMILES CS(=O)(=O)N[C@@H](CCCCN)C(=O)NC[C@H](CC1(CCCC1)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)O)C(=O)O
PubChem CID 6324648
Molecular Weight 584.68

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 100 mg/mL (171.03 mM; Need ultrasonic)

Related Documents

Solution Calculators