1. GPCR/G Protein
  2. Prostaglandin Receptor

Laropiprant (Synonyms: MK-0524)

Cat. No.: HY-50175 Purity: 99.66%
Data Sheet SDS Handling Instructions

Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).

For research use only. We do not sell to patients.
Laropiprant Chemical Structure

Laropiprant Chemical Structure

CAS No. : 571170-77-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $149 In-stock
5 mg $135 In-stock
10 mg $195 In-stock
50 mg $700 In-stock
100 mg $850 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).

IC50 & Target

Ki: 0.57 nM (DP1 receptor)

In Vitro

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[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00664287 Merck Sharp & Dohme Corp. Dyslipidemia September 2008 Phase 3
NCT01126073 University Medical Centre Ljubljana Coronary Heart Disease September 2010 Phase 4
NCT00485758 Merck Sharp & Dohme Corp. Diabetes Mellitus Type 2 July 2007 Phase 3
NCT00943124 Merck Sharp & Dohme Corp. Dyslipidemia July 2007 Phase 1
NCT01308203 Daniel A. Siniawski|Merck Sharp & Dohme Corp.|Hospital Italiano de Buenos Aires Coronary Artery Disease|Dyslipidemias October 2011 Phase 4
NCT01451619 Merck Sharp & Dohme Corp. Rosacea November 2011 Phase 1
NCT00944645 Merck Sharp & Dohme Corp. Dyslipidemia October 2006 Phase 1
NCT01228019 Merck Sharp & Dohme Corp. Hypercholesterolemia|Mixed Dyslipidemia December 2010
NCT01239992 Ludwig-Maximilians - University of Munich Hyperlipoproteinemia|Metabolic Syndrome June 2011 Phase 4
NCT01294683 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Dyslipidemia February 2011 Phase 3
NCT01683656 Calmy Alexandra|University Hospital, Geneva|Swiss National Science Foundation|Fondation Ernest Boninchi|Swiss Heart Foundation HIV|Atherosclerosis August 2012 Phase 4
NCT01274559 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Dyslipidemia March 2011 Phase 3
NCT00536510 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hyperlipidemia April 2007 Phase 3
NCT00479388 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Dyslipidemia July 2007 Phase 3
NCT01321034 Instituto Aragones de Ciencias de la Salud|Hospital Miguel Servet Hypercholesterolemia October 2011 Phase 4
NCT00618995 Merck Sharp & Dohme Corp. Type 2 Diabetes Mellitus August 2007 Phase 1
NCT00769132 Merck Sharp & Dohme Corp. Hypercholesterolemia August 2007 Phase 1
NCT01335997 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Dyslipidemia May 2011 Phase 3
NCT01012219 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Hyperlipidemia November 2009 Phase 1
NCT00269217 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Hyperlipidemia January 2006 Phase 3
NCT00378833 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hyperlipidemia July 2006 Phase 3
NCT00384293 Merck Sharp & Dohme Corp. Hypercholesterolemia, Familial September 2006 Phase 3
NCT00533312 Merck Sharp & Dohme Corp. Hypercholesterolemia April 2005 Phase 2
NCT00536237 Merck Sharp & Dohme Corp. Flushing August 2004 Phase 2
NCT00461630 University of Oxford|Merck Sharp & Dohme Corp. Cardiovascular Disease|Peripheral Arterial Disease|Diabetes Mellitus|Coronary Heart Disease January 2007 Phase 3
NCT01052311 Sheba Medical Center Coronary Artery Disease|Dyslipidemia July 2010 Phase 4
NCT00269204 Merck Sharp & Dohme Corp. Primary Hypercholesterolaemia|Mixed Hyperlipidaemia December 2005 Phase 3
NCT00111891 Merck Sharp & Dohme Corp. Dyslipidemia June 2005 Phase 2
NCT00961636 Merck Sharp & Dohme Corp. Dyslipidemia October 2009 Phase 3
NCT01054508 Central Manchester University Hospitals NHS Foundation Trust Hypercholesterolemia June 2010 Phase 4
NCT02153879 Institut Investigacio Sanitaria Pere Virgili|Spanish Biomedical Research Centre in Diabetes and Associated Metabolic Disorders Type 2 Diabetes Mellitus|Dyslipidemia February 2009 Phase 4
NCT01010516 University of Ioannina Dyslipidemia October 2009 Phase 4
NCT01071525 Rambam Health Care Campus Hypercholesterolemia April 2010 Phase 3
NCT01391377 Bayside Health|National Health and Medical Research Council, Australia Peripheral Arterial Disease July 2011
NCT01118598 Hull and East Yorkshire Hospitals NHS Trust|Merck Sharp & Dohme Corp. Polycystic Ovary Syndrome June 2010 Phase 4
NCT01583647 Merck Sharp & Dohme Corp. Hypercholesterolemia, Familial|Heterozygous Familial Hypercholesterolemia June 2012 Phase 1
NCT00479882 Merck Sharp & Dohme Corp. Primary Hypercholesterolemia|Mixed Dyslipidemia June 2007 Phase 3
NCT00289900 Merck Sharp & Dohme Corp. Mixed Hyperlipidemia January 2006 Phase 3
NCT00376584 Merck Sharp & Dohme Corp. Hypercholesteremia|Hyperlipidemia July 2006 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
References
Molecular Weight

435.9

Formula

C₂₁H₁₉ClFNO₄S

CAS No.

571170-77-9

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

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Laropiprant
Cat. No.:
HY-50175
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