ML 161

SKU: orb1225076

Description

Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.

Key Properties

• CAS Number: 423735-93-7
• MW: 361.23
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₇BrN₂O₂
• SMILES: O=C(NC1=CC=CC(NC(CCC)=O)=C1)C2=CC=CC=C2Br
• Target: PAR
• Solubility: DMSO: 72 mg/mL (199.31 mM)

Bioactivity

• In Vivo:
  Parmodulin 2 (ML161; 5 mg/kg; IV) significantly inhibits platelet thrombus formation, with a 73% inhibition in AUC (area under the curve). Parmodulin 2 inhibits platelet thrombus formation In vivo, and it does not prolong bleeding time. Parmodulin 2 selectively inhibits platelet aggregation through Par1 and the α2A-adrenergic receptor. Animal model: C57BL/6J wild type mice. Dosage: 5 mg/kg (Pharmacokinetic Analysis). Administration: IV. Result: Significantly inhibited platelet thrombus formation, with a 73% inhibition in AUC.
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• In Vitro:
  Parmodulin 2 (ML161; 10 μM; for 30 minutes) inhibits proinflammatory signaling in endothelial HUVECs cells.

Storage & Handling

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

Alternative Names

AG-670 | CID-1048267

Quick Database Links

Gene Symbol

PAR