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Merck
모든 사진(1)

문서

SML2893

Sigma-Aldrich

LIT-927

≥98% (HPLC)

동의어(들):

4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-2(1H)-pyrimidinone, 4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)pyrimidin-2(1H)-one

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About This Item

실험식(Hill 표기법):
C17H13ClN2O3
CAS Number:
Molecular Weight:
328.75
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

yellow to brown

solubility

DMSO: 2 mg/mL, clear (warmed)

저장 온도

2-8°C

SMILES string

O=C1N=C(C=C(N1)C2=CC=C(C(OC)=C2)O)C3=CC=C(C=C3)Cl

생화학적/생리학적 작용

LIT-927 is an orally active CXCL12 (SDF1) neutraligand (Kd = 267) that selectively neutralizes CXCL12, but not CCL17, CCL22, CCL5, or CCL2 activity in cultures (10 μM LIT-927 against 5 nM chemokine-induced calcium mobilization). LIT-927 reduces eosinophil recruitment in a murine allergic airway hypereosinophilia model in vivo (330 nmol/kg intranasal, 350 nmol/kg ip. or 1400 μmol/kg po.), offering greatly improved oral activity and solubility than Chalcone-4, and exhibiting little side-effects when compared with dexamethasone or CXCR4 antagonist AMD3100.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Jennifer Bordenave et al.
Cardiovascular research, 116(3), 686-697 (2019-06-08)
The progressive accumulation of cells in pulmonary vascular walls is a key pathological feature of pulmonary arterial hypertension (PAH) that results in narrowing of the vessel lumen, but treatments targeting this mechanism are lacking. The C-X-C motif chemokine 12 (CXCL12)
Pierre Regenass et al.
Journal of medicinal chemistry, 61(17), 7671-7686 (2018-08-15)
We previously reported Chalcone-4 (1) that binds the chemokine CXCL12, not its cognate receptors CXCR4 or CXCR7, and neutralizes its biological activity. However, this neutraligand suffers from limitations such as poor chemical stability, solubility, and oral activity. Herein, we report

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