产品说明书
LIT-927
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同义名 : | - |
| CAS号 : | 2172879-52-4 | |
| 货号 : | A914195 | |
| 分子式 : | C17H13ClN2O3 | |
| 纯度 : | 98% | |
| 分子量 : | 328.75 | |
| MDL号 : | MFCD31726172 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(36.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The chemokine receptor CXCR4 and its ligand CXCL12 are involved in the progression and dissemination of a diverse number of solid and hematological malignancies. Binding CXCL12 to CXCR4 activates a variety of intracellular signal transduction pathways that regulate cell chemotaxis, adhesion, survival, proliferation, and apoptosis[1]. LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to its specific receptor CXCR4[2]. LIT-927 is selected as lead neutraligand and characterized its activity (IC50) in vivo in a dose–response efficacy study on eosinophil recruitment in mouse model. LIT-927 at 10 μM is able to inhibit the increase in intracellular calcium concentration in EGFP-CXCR4+ HEK cells in response to CXCL12, while it has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CXCR4+ HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or CCL2 on EGFP-CCR2+ HEK cells. These results demonstrate the high selectivity of LIT-927 toward CXCL12 vs other chemokines also involved in asthma[2]. More interestingly, LIT-927 displayed very good to excellent in vivo activity, inhibiting eosinophil infiltration by 48%[2]. LIT-927 reduced eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 was the only one to display inhibitory activity following oral administration[2]. | ||
| 作用机制 | Docking of LIT-927 to this pocket at the vicinity of Trp57 is possible at the condition to allow side-chain flexibility for three residues (Arg20, Trp57, and Tyr61) that would control the entry to the Trp57 pocket. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.04mL 0.61mL 0.30mL |
15.21mL 3.04mL 1.52mL |
30.42mL 6.08mL 3.04mL |
| 参考文献 |
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