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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally bioavailable D prostanoid receptor 2 (DP2, formerly 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 prevents T helper 2 lymphocytes and eosinophils from being activated in a mast cell-dependent manner. With Ki values of 4nM and 3nM, OC000459, an antagonist of DP2, can stop PGD2 from binding to both human DP2 and rat recombinant DP2. Treatment with OC000459 prevented LAR and the rise in sputum eosinophils following an allergen. In asthma, OC000459 seems to reduce allergic inflammation. When compared to human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM), timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2. Timapiprant sodium (OC000459 sodium) prevents Th2 lymphocytes and eosinophils from being activated by mast cells.
| Targets |
human recombinant DP2 ( Ki = 0.013 μM ); rat recombinant DP2 ( Ki = 0.003 μM ); human native DP2 ( Ki = 0.004 μM )
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| Cell Assay |
Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits human Th2 lymphocyte chemotaxis (IC50=0.028 μM) and cytokine production (IC50=0.019 μM). The activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells is inhibited by timapiprant (OC000459) (1 μM).
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| References |
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| Molecular Formula |
C21H16FN2NAO2
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|---|---|
| Molecular Weight |
370.35
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| Exact Mass |
370.11
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| Elemental Analysis |
C, 68.10; H, 4.35; F, 5.13; N, 7.56; Na, 6.21; O, 8.64
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| CAS # |
950688-14-9
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| Related CAS # |
Timapiprant; 851723-84-7
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C2=C(N1CC(=O)[O-])C=CC(=C2)F)CC3=NC4=CC=CC=C4C=C3.[Na+]
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| InChi Key |
XKRNYIKRDAGPQZ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C21H17FN2O2.Na/c1-13-17(11-16-8-6-14-4-2-3-5-19(14)23-16)18-10-15(22)7-9-20(18)24(13)12-21(25)26;/h2-10H,11-12H2,1H3,(H,25,26);/q;+1/p-1
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| Chemical Name |
2-[5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetate
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| Synonyms |
OC000459 sodium; OC000459; OC-000459; OC 000459; Timapiprant; Timapiprant sodium
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~270.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7001 mL | 13.5007 mL | 27.0015 mL | |
| 5 mM | 0.5400 mL | 2.7001 mL | 5.4003 mL | |
| 10 mM | 0.2700 mL | 1.3501 mL | 2.7001 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01448902 | Completed | Drug: OC000459 Drug: Placebo |
Allergic Rhinitis | Oxagen Ltd | March 2007 | Phase 2 |
| NCT01056575 | Completed | Drug: OC000459 | Healthy Volunteers | Oxagen Ltd | February 2010 | Phase 1 |
| NCT01056783 | Completed | Drug: OC000459 Drug: Placebo |
Eosinophilic Esophagitis | Oxagen Ltd | August 2010 | Phase 2 |
| NCT02341521 | Completed | Drug: OC000459 | Asthma | Atopix Therapeutics, Ltd. | March 2015 | Phase 1 |
| NCT02002208 | Completed | Drug: OC000459 | Atopic Dermatitis | Atopix Therapeutics, Ltd. | October 2013 | Phase 2 |
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