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| LaropiprantDP1 receptor antagonist,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
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| Cas No. | 571170-77-9 | SDF | Download SDF |
| Synonyms | 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 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Laropiprant(Cardaptive; MK 0524) is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 μM for the DP1 and DP2 receptors, respectively. Laropiprant(Cardaptive; MK 0524) inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively. In a sheep model of allergic rhinitis, 0.1 mg/kg MK 0524 completely blocked PGD2-induced nasal congestion. At a dose of 4 mg/kg, MK 0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a murine model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.
