A CRTH2/DP2 antagonist
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LAS191859

Item No. 20238

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[[(cyclopropylcarbonyl)ethylamino]methyl]-4-(trifluoromethyl)phenyl]-6-methyl-1H-pyrrolo[2,3-b]pyridine-3-acetic acid
CAS Number
1420071-13-1
Molecular Formula
C24H24F3N3O3
Formula Weight
459.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 2.5 mg/ml
λmax
272 nm
SMILES
CCN(C(C1CC1)=O)CC2=CC(C(F)(F)F)=CC=C2N3C=C(CC(O)=O)C4=C3N=C(C)C=C4
InChi Code
InChI=1S/C24H24F3N3O3/c1-3-29(23(33)15-5-6-15)12-17-10-18(24(25,26)27)7-9-20(17)30-13-16(11-21(31)32)19-8-4-14(2)28-22(19)30/h4,7-10,13,15H,3,5-6,11-12H2,1-2H3,(H,31,32)
InChi Key
KGBYKYDRYYERIX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $174

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    1 mg

    $312

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    Product Description

    LAS191859 is a potent antagonist of CRTH2/DP2 with IC50 values of 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively.1 It is selective for CRTH2/DP2 over a panel of 65 enzymes, ion channels, and transporters with <25% inhibition for all targets when tested at a concentration of 10 μM. LAS191859 reduces shape change of eosinophils (IC50s = 2 and 8.2 nM in isolated eosinophils and whole blood, respectively) and eosinophil chemotaxis (IC50 = 1.3 nM) induced by prostaglandin D2 (PGD2; Item No. 12010) binding to CRTH2/DP2. Oral administration of LAS191859 reduces PGD2-induced systemic eosinophilia in guinea pigs (ID50 = 131 μg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Calbet, M., Andrés, M., Armengol, M., et al. Pharmacological characterization of CRTh2 antagonist LAS191859: Long receptor residence time translates into long-lasting in vivo efficacy. Pharmacol. Res. 111, 208-216 (2016).