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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 572874-50-1
- Formule: C21H18ClFNNaO4S
- Masse moléculaire:457.88
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 572874-50-1
-
Masse moléculaire 457.88
-
Formule C21H18ClFNNaO4S
-
SMILES
O=S(C1=CC(F)=CC2=C1N(C3=C2CC[C@@H]3CC(O[Na])=O)CC4=CC=C(Cl)C=C4)(C)=O
-
Synonyms
MK-0524 sodium
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Powered by Bioz