Saralasin acetate(34273-10-4 free base)

SKU: orb1218067

Description

Saralasin acetate is a Non-selective angiotensin II antagonist.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 39698-78-7
• MW: 990.11
• Purity: >98% (HPLC)
• Formula: C₄₄H₇₁N₁₃O₁₃
• SMILES: CC(C)[C@@H](C(N[C@@H](Cc1cnc[nH]1)C(N(CCC1)[C@@H]1C(N[C@@H](C)C(O)=O)=O)=O)=O)NC([C@H](Cc(cc1)ccc1O)NC([C@H](C(C)C)NC([C@H](CCCN=C(N)N)NC(CNC)=O)=O)=O)=O.CC(O)=O.O
• Target: RAAS

Bioactivity

• In Vivo:
  Saralasin acetate hydrate (intravenous injection, 5-50 μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis. Saralasin acetate hydrate (subcutaneous injection, 10 and 30 mg/kg, a single dose) increases serum renin activity (SRA) in normal, conscious rats, without markedly altering blood pressure or heart rate. Animal model: Cerulein-induced acute pancreatitis rats model. Dosage: 5, 10, 20, and 50 μg/kg, a single dose. Administration: Intravenous injection. Result: Restored the pancreatic morphological characteristics to the control level. Reduced pancreatic injury and suppressed the glutathione depletion induced by cerulean. Animal model: Male Sprague-Dawley rats. Dosage: 10 and 30 mg/kg, a single dose. Administration: Subcutaneous injection. Result: Stimulated renin release without altering blood pressure or heart rate at the time of measuring serum renin levels 20 minutes after injection.
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• In Vitro:
  Saralasin acetate hydrate (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells. Saralasin acetate hydrate (5 μM, 2h) restores Ito, fast (Fast-Inactivating Transient Outward K+ Current in Mouse Ventricle) and I K, slow (Slow-Inactivating Transient Outward K+ Current in Mouse Ventricl) to control levels in myocytes. Saralasin acetate hydrate (0.1-10 nM, 40 min) inhibits binding of FITC-Ang II to rat liver membrane preparation (used as the source of angiotensin receptors) with a Ki value of 0.32 nM for 74% of the binding sites and 2.7 nM for the remaining binding sites. Saralasin acetate hydrate (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels. Cell Proliferation Assay Cell line: 3T3 and SV3T3 cells. Concentration: 1 nM. Incubation time: 48 h, 72 h. Result: Inhibited cell growth in 3T3 and SV3T3 cells and caused an increase of cellular renin concentration.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

RAAS