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Laropiprant
CAS No. 571170-77-9
Laropiprant( MK 0524 | MK-0524 )
Catalog No. M15081 CAS No. 571170-77-9
A potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 70 | In Stock |
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| 5MG | 119 | In Stock |
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| 10MG | 173 | In Stock |
|
| 25MG | 347 | In Stock |
|
| 50MG | 533 | In Stock |
|
| 100MG | 761 | In Stock |
|
| 500MG | 1521 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameLaropiprant
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NoteResearch use only, not for human use.
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Brief DescriptionA potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM.
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DescriptionA potent and selective prostaglandin D2 (PGD2) receptor (DP1) antagonist with Ki of 0.57 nM; shows weaker affinity for TP (Ki=2.95 nM), no significant activity on EP1, EP2, EP3, EP4, FP, and IP; inhibits the accumulation of cAMP in washed platelets and in plateletrich plasma challenged with PGD with IC50 of 0.09 nM and 4 nM, respectively; displays an excellent rat pharmacokinetic profile and efficacious in a sheep model of allergic rhinitis.Dyslipidemia Withdrawn.
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In VitroLaropiprant (0.01-1000 μM; 10 mins; HEK293 cells) is an inverse agonist of DP1 cAMP signaling and reduces DP1 cAMP signaling below basal levels.Laropiprant (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression.
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In VivoLaropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles.Pharmacokinetic Analysis in Male Sprague-Dawley rats.
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SynonymsMK 0524 | MK-0524
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PathwayGPCR/G Protein
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TargetProstaglandin Receptor
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RecptorProstaglandin Receptor
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Research AreaCardiovascular Disease
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IndicationDyslipidemia
Chemical Information
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CAS Number571170-77-9
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Formula Weight435.8963
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Molecular FormulaC21H19ClFNO4S
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(O)C[C@H]1CCC2=C1N(CC3=CC=C(Cl)C=C3)C4=C2C=C(F)C=C4S(=O)(C)=O
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Chemical NameCyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Sturino CF, et al. J Med Chem. 2007 Feb 22;50(4):794-806.
2. Cheng K, et al. Proc Natl Acad Sci U S A. 2006 Apr 25;103(17):6682-7.
3. Philip G, et al. J Allergy Clin Immunol. 2009 Nov;124(5):942-8.e1-9.
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