1. Metabolic Enzyme/Protease
  2. Neprilysin
  3. SQ28603

SQ28603 (Synonyms: SQ28,603; Squibb 28603)

Cat. No.: HY-U00171
Handling Instructions

SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).

For research use only. We do not sell to patients.

SQ28603 Chemical Structure

SQ28603 Chemical Structure

CAS No. : 100845-83-8

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Description

SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).

IC50 & Target

NEP[1]

In Vivo

In conscious deoxycorticosterone acetate (DOCA)/salt hypertensive rats, 300 μmol/kg, i.v., of SQ28603 significantly lowers mean arterial pressure (MAP) from 177±12 to 154±8 mm Hg and increases urinary cyclic guanosine monophosphate (GMP) excretion from 204±70 to 1,068±326 pmol/kg/min within 2 h. SQ28603 also significantly reduces NEP activity by 95% in the kidneys (1.28±0.08 vs. 18.35±0.61 μmol/min after SQ28603 and vehicle respectively) and by 77% in the lungs (0.29±0.03 vs. 0.92±0.14 μmol/kg after SQ28603 and vehicle, respectively). In conclusion, inhibition of NEP activity by SQ28603 significantly decreases MAP and increases plasma ANP concentrations and urinary excretion of cyclic GMP in conscious DOCA/salt hypertensive rats[1]. The potent neutral endopeptidase inhibitor SQ28603 significantly increases excretion of sodium from 4.9±2.3 to 14.3±2.1 muequiv./min and cyclic 3',5'-guanosine monophosphate from 118±13 to 179±18 pmol/min after intravenous administration of 300 μmol/kg (approximately 80 mg/kg) in conscious female cynomolgus monkeys[2].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

267.34

Formula

C₁₃H₁₇NO₃S

CAS No.

100845-83-8

SMILES

OC(CCNC(C(CS)CC1=CC=CC=C1)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere

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SQ28603
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SQ28603

Cat. No.: HY-U00171