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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
yellow to brown
溶解度
DMSO: 2 mg/mL, clear (warmed)
儲存溫度
2-8°C
SMILES 字串
O=C1N=C(C=C(N1)C2=CC=C(C(OC)=C2)O)C3=CC=C(C=C3)Cl
生化／生理作用
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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