Laropiprant

SKU: orb1308138

Description

Laropiprant (MK-0524) is a potent, selective antagonist of the prostaglandin D2 receptor DP1 (Ki = 0.57 nM) with additional activity at the TP receptor (Ki = 2.95 nM). This small molecule is a valuable research tool for investigating the roles of PGD2 signaling in allergic responses, inflammation, and cardiovascular research in both in vitro and in vivo models.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 571170-77-9
• MW: 435.9
• Purity: 99.97% (May vary between batches)
• Formula: C₂₁H₁₉ClFNO₄S
• SMILES: CS(=O)(=O)c1cc(F)cc2c3CC[C@H](CC(O)=O)c3n(Cc3ccc(Cl)cc3)c12
• Target: Prostaglandin Receptor
• Solubility: DMSO:100 mg/mL (229.41 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.18 mM)

Bioactivity

• Target IC50:
  TP receptor:2.95 nM (ki)|DP/DP1 receptor:0.57 nM (ki)
• In Vitro:
  Laropiprant blocks DP receptor-dependent enhance in VASP phosphorylation, as well as inhibition of P-selectin expression, GPIIb/IIIa activation, and in vitro thrombus formation. Laropiprant antagonizes the increased platelet aggregation by TP and EP3 receptor activation. Laropiprant (1 μM) induces a significant inhibition of the aggregation but still counteracts the pronounced inhibition caused by PGD2 (30 nM) and BW245c (3 nM). Laropiprant (10 μM) and niacin inhibit in vitro thrombus formation.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

metabolismacyl, MK 0524, MK0524, MK-0524, inhibit, Inhibitor, Laropiprant, glucuronide, DP/DP1 Receptor, DP receptor, pharmacokinetics, TP Receptor, ProstaglandinReceptor, Prostaglandin Receptor

Compound Identifiers

PubChem CID

9867642