Laropiprant (Synonyms: Cardaptive; MK 0524; MK-0524,Laropiprant ) |
| رقم الكتالوجGC11833 |
A potent, selective DP1 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 571170-77-9
Sample solution is provided at 25 µL, 10mM.
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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.
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].
Reference：
[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.
Cell experiment: | 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. | |
| Cas No. | 571170-77-9 | SDF | |
| المرادفات | Cardaptive; MK 0524; MK-0524,Laropiprant | ||
| Chemical Name | 2-[(3R)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1H-cyclopenta[b]indol-3-yl]acetic acid | ||
| Canonical SMILES | CS(=O)(=O)C1=C2C(=CC(=C1)F)C3=C(N2CC4=CC=C(C=C4)Cl)C(CC3)CC(=O)O | ||
| Formula | C21H19ClFNO4S | M.Wt | 435.9 |
| الذوبان | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2941 mL | 11.4705 mL | 22.941 mL |
| 5 mM | 0.4588 mL | 2.2941 mL | 4.5882 mL |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2941 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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