LAS191859 | CAS:1420071-13-1

• 価格
• 構造式
• 製品情報
• 製品詳細
• 文献

価格

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構造式

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製品情報

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. It is selective for CRTH2/DP₂ over a panel of 65 enzymes, ion channels, and transporters with 50s = 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).

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製品詳細

name	LAS191859
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	A crystalline solid
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
Storage	-20°C
Shipping	Wet ice in continental US; may vary elsewhere
Stability	≥ 2 years

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文献

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).

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