产品说明书
BX471 HCl
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同义名 : | ZK-811752 hydrochloride;BX471 hydrochloride |
| CAS号 : | 288262-96-4 | |
| 货号 : | A151361 | |
| 分子式 : | C21H25Cl2FN4O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 471.353 | |
| MDL号 : | MFCD28167805 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 115 mg/mL(243.98 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 | |||
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| 描述 | The CC chemokine receptor 1 (CCR1) is a therapeutic target for the treatment of autoimmune diseases. BX471 HCl is a non-peptide CCR1 antagonist that displaces the CCR1 ligands, including MIP-1α, RANTES, and MCP-3, with high affinity (Ki = 1.0, 2.8, and 5.5 nM, respectively). It also dose-dependently inhibited Ca2+ mobilization induced by MIP-1α (30 nM), RANTES (300 nM), and MCP-3 (100 nM) with IC50 values of 5, 2, and 6 nM, respectively. The increase in the intracellular Ca2+ concentration by 30 nM MIP-1α was completed inhibited by BX471 HCl at a dosage of 300 nM. BX471 HCl at 1 μM inhibited MIP-1α-induced upregulation of CD11b in human blood[3]. The treatment with 20 mg/kg BX471 HCl for 10 days resulted in 55% reduction of interstitial CD45 positive leukocytes in a mouse model of unilateral ureter obstruction (UUO). BX471 HCl-treated mice also showed significantly decreased CCR5-positive CD8 T cells in UUO kidneys as compared with the vehicle controls (44.2% vs. 64.3%). Additionally, BX471 HCl reduced the amount of FSP1-positive cells by 65% in UUO kidneys compared with the vehicle-treated group[4]. | ||
| 作用机制 | BX 471 is a potent inhibitor of chemokine binding to CCR. It blocks CCR1 activation as depicted by the inhibition of Ca2+ mobilization, CD11b expression, extracellular acidification and cell migration[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.61mL 2.12mL 1.06mL |
21.22mL 4.24mL 2.12mL |
| 参考文献 |
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