A potent, selective DP2 antagonist
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OC000459

Item No. 12027

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-2-methyl-3-(2-quinolinylmethyl)-1H-indole-1-acetic acid
CAS Number
851723-84-7
Molecular Formula
C21H17FN2O2
Formula Weight
348.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.5 mg/mlDMSO: 1.1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
229, 281, 318 nm
SMILES
FC1=CC=C(N(CC(O)=O)C(C)=C2CC3=CC=C(C=CC=C4)C4=N3)C2=C1
InChi Code
InChI=1S/C21H17FN2O2/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)
InChi Key
FATGTHLOZSXOBC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $75

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    10 mg

    $128

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    25 mg

    $259

    Add
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    Product Description

    OC000459 is a potent, selective DP2 antagonist that displaces [3H]prostaglandin D2 ([3H]PGD2) from human recombinant DP2 receptors (Ki = 13 nM), rat recombinant DP2 receptors (Ki = 3 nM), and human native DP2 (Ki = 4 nM; Th2 cell membranes) without interfering with the ligand binding properties of other prostanoid receptors, including PGE1–4, DP1, TP, PGI2, and PGF.1 OC000459 inhibits chemotaxis and cytokine production of human Th2 lymphocytes with IC50 values of 28 and 19 nM, respectively, and competitively antagonizes eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5).1 OC000459 was shown to inhibit blood eosinophilia in rats induced by 13,14-dihydro-15-keto PGD2 (Item No. 12610) (ED50 = 0.04 mg/kg) and airway eosinophilia in guinea pigs in response to an aerosol of 13,14-dihydro-15-keto PGD2 (ED50 = 0.01 mg/kg).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1.  .