OC000459 |
| Katalog-Nr.GC12536 |
Antagonist of D prostanoid receptor 2 ,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 851723-84-7,950688-14-9
Sample solution is provided at 25 µL, 10mM.
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OC000459 is a potent, selective and orally active antagonist of D prostanoid receptor 2 (DP2) with Ki value of 4nM [1].
DP2 is expressed on Th2 cells and eosinophils. It is activated by PGD2 which is reported to have effects on the pathogenesis of allergic disease. 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. In CHO cells expressing DP2, OC000459 suppresses PGD2 mediated calcium mobilization with IC50 value of 28nM. In human Th2 cells, OC000459 inhibits chemotaxis and production of IL-13 in response to PGD2 with IC50 values of 28nM and 19nM. In addition, oral administration of OC000459 effectively reduces blood eosinophilia in rats. OC000459 also shows inhibitory effect on the accumulation of eosinophil in guinea pigs aerosolized by DK-PGD2. Furthermore, OC000459 is also reported to inhibit the late-phase allergic response in patients with asthma [1, 2].
References:
[1] Pettipher R, Vinall S L, Xue L, et al. 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. Journal of Pharmacology and Experimental Therapeutics, 2012, 340(2): 473-482.
[2] Singh D, Cadden P, Hunter M, et al. Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. European Respiratory Journal, 2013, 41(1): 46-52.
| Cas No. | 851723-84-7,950688-14-9 | SDF | |
| Chemical Name | 2-[5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetic acid | ||
| Canonical SMILES | CC1=C(C2=C(N1CC(=O)O)C=CC(=C2)F)CC3=NC4=CC=CC=C4C=C3 | ||
| Formula | C21H17FN2O2 | M.Wt | 348.37 |
| Löslichkeit | DMF: 0.5 mg/ml,DMSO: 1.1 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 | 5.741 mL |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8705 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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