| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Timapiprant (formerly known as OC000459; OC-000459) is a novel, potent, selective, and orally bioactive prostanoid receptor 2 (DP2- also known as CRTH2)) antagonist with IC50 of 13 nM. It 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. As an antagonist of DP2, OC000459 can prevent PGD2 from binding to human DP2 and rat recombinant DP2 with Ki values of 4nM and 3nM. OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils. OC000459 appears to inhibit allergic inflammation in asthma.
| ln Vitro |
Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) suppresses human Th2 cells' chemotaxis (IC50=0.028 μM) and their production of cytokines (IC50=0.019 μM)[1]. Timapiprant (OC000459) (1 μM) prevents Th2 cells and eosinophils from becoming activated in reaction to IgE/anti-IgE-stimulated human mast cell supernatants[1]. With an IC50 of 0.035 uM, timapiprant (OC000459) (1 nM–1000 nM; 16 hours) suppresses PGD2's anti-apoptotic action on Th2 cells[1].
|
||
|---|---|---|---|
| ln Vivo |
In rats (ED50=0.04 mg/kg), timapiprant (OC000459) (gavage; 2 mg/kg, 10 mg/kg) reduces blood eosinophilia caused by 13,14-dihydro-15-keto-PGD2 (DK-PGD2)[1]. In reaction to an aerosol of DK-PGD2, timapiprant (OC000459) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) reduces airway eosinophilia in guinea pigs (ED50=0.01 mg/kg)[1].
|
||
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: Th2 Cells Tested Concentrations: 0.0001 μM-10 μM Incubation Duration: 16 hrs (hours) Experimental Results: Inhibited the antiapoptotic effect of PGD2. |
||
| Animal Protocol |
|
||
| References |
[1]. 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
|
| Molecular Formula |
C21H17FN2O2
|
|
|---|---|---|
| Molecular Weight |
348.37
|
|
| CAS # |
851723-84-7
|
|
| Related CAS # |
Timapiprant sodium;950688-14-9
|
|
| SMILES |
O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4
|
|
| Chemical Name |
2-(5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)-1H-indol-1-yl)acetic acid
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8705 mL | 14.3526 mL | 28.7051 mL | |
| 5 mM | 0.5741 mL | 2.8705 mL | 5.7410 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8705 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA