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.
For research use only. We do not sell to patients.
- CAS No.: 572874-50-1
- Formula: C21H18ClFNNaO4S
- Molecular Weight:457.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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DP 0.57 nM (Ki) |
TP 2.95 nM (Ki) |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 572874-50-1
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Molecular Weight 457.88
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Laropiprant sodium Related Classifications
HY-50175A Related Classifications
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