Timapiprant sodium manufacturers
|
| | Timapiprant sodium Basic information |
| Product Name: | Timapiprant sodium | | Synonyms: | Timapiprant sodium;Timapiprant Sodium (OC000459 Sodium);OC000459 SODIUM;Timapiprant sodium (OC000459);Timapiprant (sodium salt) | | CAS: | 950688-14-9 | | MF: | C21H18FN2NaO2 | | MW: | 372.38 | | EINECS: | | | Product Categories: | | | Mol File: | 950688-14-9.mol |  |
| | Timapiprant sodium Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 100 mg/mL (270.01 mM) | | form | Solid | | color | Light yellow to yellow |
| | Timapiprant sodium Usage And Synthesis |
| Description | Timapiprant, also known as OC000459, is a potent, selective and orally active CRTH2 antagonist. OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. OC000459 inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils. OC000459 appears to inhibit allergic inflammation in asthma. | | Uses | Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1]. | | in vivo | Timapiprant sodium (OC000459 sodium) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50=0.04 mg/kg)[1].
Timapiprant sodium (OC000459 sodium) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50=0.01 mg/kg)[1]. | | References | [1] Singh D, Cadden P, Hunter M, Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. Eur Respir J. 2013 Jan;41(1):46-52. DOI:10.1183/09031936.00092111
[2] Horak F, Zieglmayer P, Zieglmayer R, The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. Allergy. 2012 Dec;67(12):1572-9. DOI:10.1111/all.12042
[3] Pettipher R, Vinall SL, Xue L, Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J Pharmacol Exp Ther. 2012 DOI:10.1124/jpet.111.187203 |
| | Timapiprant sodium Preparation Products And Raw materials |
|