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Postion:Product Catalog >Laropiprant
Laropiprant
  • Laropiprant

Laropiprant

Price $1
Package 1g
Min. Order: 1g
Supply Ability: 1ton
Update Time: 2020-01-13

Product Details

Product Name: Laropiprant CAS No.: 571170-77-9
EC-No.: 200-258-5 Min. Order: 1g
Purity: 99% Supply Ability: 1ton
Release date: 2020/01/13
contact: Mary@coreychem.com
Common Name
Laropiprant
CAS Number
571170-77-9
Molecular Weight
435.896
Density
1.5±0.1 g/cm3
Boiling Point
710.0±60.0 °C at 760 mmHg
Molecular Formula
C21H19ClFNO4S
Melting Point
175∶ºC
MSDS
N/A
Flash Point
383.2±32.9 °C

 Use of Laropiprant

 
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.

 Names

Name
2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid
Synonym
More Synonyms

 Laropiprant Biological Activity

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.
Related Catalog
Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Research Areas >> Inflammation/Immunology
Target

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].
Cell Assay
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].
References

[1]. Sturino CF, et al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806.

[2]. Philipose S, et al. Laropiprant Attenuates EP3 and TP Prostanoid Receptor-Mediated Thrombus Formation. PLoS One. 2012;7(8):e40222.

 Chemical & Physical Properties

Density
1.5±0.1 g/cm3
Boiling Point
710.0±60.0 °C at 760 mmHg
Melting Point
175∶ºC
Molecular Formula
C21H19ClFNO4S
Molecular Weight
435.896
Flash Point
383.2±32.9 °C
Exact Mass
435.070740
PSA
84.75000
LogP
3.82
Vapour Pressure
0.0±2.4 mmHg at 25°C
Index of Refraction
1.664

 Synonyms

Laropiprant
Laropiprant (INN/USAN)
Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-
[(3R)-4-(4-chlorophenyl)methyl-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b] indol-3-yl]acetic acid
(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta(b)indol-3-yl acetic acid
cc-711
(3R)-[4-(4-chlorobenzyl)-7-fluoro-5-(methane-sulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
(-)-[4-(4-chlorobenzyl)-7-fluoro-5-(methanesulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]-indol-3-yl]acetic acid
MFCD11042421
[(3R)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
[14C]-Laropiprant
MK 0524
UNII-G7N11T8O78

Company Profile Introduction

Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals. Mainly deals in the sales of: Pharmaceutical intermediates OLED intermediates: Pharmaceutical intermediates; OLED intermediates;

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