1. GPCR/G Protein
  2. Prostaglandin Receptor

Laropiprant (Synonyms: MK-0524)

Cat. No.: HY-50175 Purity: 99.21%
Handling Instructions

Laropiprant is a potent, selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

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

Laropiprant Chemical Structure

Laropiprant Chemical Structure

CAS No. : 571170-77-9

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10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 234 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Laropiprant is a potent, selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

IC50 & Target[1]

DP/DP1 Receptor

0.57 nM (Ki)

TP Receptor

2.95 nM (Ki)

In Vitro

Laropiprant is a potent, selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.[1]. Laropiprant (1 µM) causes a significant inhibition of the aggregation but still counteractes the pronounced inhibition caused by PGD2 (30 nM) and BW245c (3 nM). Laropiprant blocks DP receptor-dependent increase 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 (10 µM) and niacin inhibit in vitro thrombus formation[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2941 mL 11.4705 mL 22.9410 mL
5 mM 0.4588 mL 2.2941 mL 4.5882 mL
10 mM 0.2294 mL 1.1471 mL 2.2941 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Vena8Fluoro+ Biochips are coated with collagen (200 µg/mL) at 4°C overnight and thereafter blocked with bovine serum albumin (10 µg/mL) for 30 minutes at room temperature followed by washing steps. Whole blood collected in sodium citrate is incubated with 3, 3-dihexyloxacarbocyanine iodide (1 µM) in the dark for 10 minutes. PGD2 (30 nM), BW245c (3 nM) are added 10 min before the start of perfusion, and the DP antagonist BWA868c or Laropiprant (1 µM) are added 10 min before the agonists. In another set of experiments whole blood is treated with niacin (3 mM), acetylsalicylic acid (1 mM) or Laropiprant (1 µM and 10 µM) for 30 min. CaCl2 at a final concentration of 1 mM is added 2 minutes before the perfusion over the collagen-coated chip. Perfusion is carried out at a shear rate of 30 dynes cm2. Thrombus formation is recorded. Computerized image analysis is performed by DucoCell analysis software, where the area covered by the thrombus is calculated. Data are expressed as percent of area covered in a control sample[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

435.90

Formula

C₂₁H₁₉ClFNO₄S

CAS No.

571170-77-9

SMILES

O=S(C1=CC(F)=CC2=C1N(C3=C2CC[[email protected]@H]3CC(O)=O)CC4=CC=C(Cl)C=C4)(C)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Laropiprant
Cat. No.:
HY-50175
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Laropiprant

Cat. No.: HY-50175