Laropiprant sodium
Laropiprant sodium is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.
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- CAS. Nr.: 572874-50-1
- Formel: C21H18ClFNNaO4S
- Molecular Weight:457.88
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
DP 0.57 nM (Ki) |
TP 2.95 nM (Ki) |
In Vitro
Laropiprant sodium (0.01-1000 μM; 10 mins; HEK293 cells) is an Inverse Agonist of DP1 cAMP Signaling and reduces DP1 cAMP signaling below basal levels[1].
Laropiprant sodium (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pharmacokinetic Analysis in Male Sprague-Dawley rats[3]
| Route | Dose (mg/kg) | AUC0-∞ (μM·hr) | Clp (mL/min/kg) | Vdss (L/kg) | T1/2 (hr) |
| PO | 1 | 22.7 | 1.9 | 0.7 | 7.4 |
| PO | 5 | 96.0 | 2.1 | 0.9 | 7.6 |
| Route | Dose (mg/kg) | AUC0-∞ (μM·hr) | Cmax (μM) | Tmax (hr) | F(%) |
| IV | 5 | 52.6 | 15.6 | 1.2 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 572874-50-1
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Molecular Weight 457.88
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Formel C21H18ClFNNaO4S
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SMILES
O=S(C1=CC(F)=CC2=C1N(C3=C2CC[C@@H]3CC(O[Na])=O)CC4=CC=C(Cl)C=C4)(C)=O
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Synonyms
MK-0524 sodium
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[2]. 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. [Content Brief]
[3]. Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Laropiprant sodium Related Classifications
HY-50175A Related Classifications
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