A CRTH2/DP2 receptor antagonist
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MK-7246

Item No. 34208

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(7R)-7-[[(4-fluorophenyl)sulfonyl]methylamino]-6,7,8,9-tetrahydro-pyrido[1,2-a]indole-10-acetic acid
CAS Number
1218918-62-7
Molecular Formula
C21H21FN2O4S
Formula Weight
416.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/ml
SMILES
OC(CC1=C2N(C[C@@H](CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=CC=CC=C41)=O
InChi Code
InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-21(25)26)17-4-2-3-5-19(17)24(20)13-15/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)/t15-/m1/s1
InChi Key
JTCAGRAKUAAYDY-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $70

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    5 mg

    $278

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    10 mg

    $486

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    25 mg

    $953

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    Product Description

    MK-7246 is an antagonist of the prostaglandin D2 (PGD2; Item No. 12010) receptor CRTH2/DP2 (Ki = 2.5 nM).1 It is selective for CRTH2/DP2 over DP1, the PGF2α receptor (FP), the PGI2 receptor (IP), and the thromboxane A2 (TP) receptor (Kis = 373, >25,100, >23,030, and 3,804 nM, respectively), as well as the PGE2 receptor subtypes 1-4 (EP1-4; Kis = 7,668-23,330 nM). MK-7246 inhibits 13,14-dihydro-15-keto-PGD2-induced inhibition of cAMP formation in HEK293 cells expressing human CRTH2/DP2 (IC50 = 3 nM). It also inhibits 13,14-dihydro-15-keto-PGD2-induced eosinophil shape change (IC50 = 2.2 nM) and CD11b upregulation on eosinophils and basophils in isolated human whole blood (IC50s = 6.2 and 5.4 nM, respectively). MK-7246 (1 mg/kg) decreases antigen-induced late-phase bronchoconstriction and completely prevents airway hyperresponsiveness in sheep.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gervais, F.G., Sawyer, N., Stocco, R., et al. Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist. Mol. Pharmacol. 79(1), 69-76 (2011).