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抑制剂/激活剂

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凋亡与自噬

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Reparixin L-lysine salt

Reparixin L-lysine salt Repertaxin L-lysine salt

Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化的变构抑制剂。

货号：
TK0593
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	266359-93-7
生物活性	Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
分子式	C20H35N3O5S
分子量	429.57
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	H2O : 100 mg/mL (232.79 mM; Need ultrasonic) DMSO : 100 mg/mL (232.79 mM; Need ultrasonic)
体内研究	The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50 µg/mL, but lower at higher concentrations. Although radioactivity is rapidly distributed into rat tissues, Vss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t1/2~0.5 h) than in dogs (t1/2~10 h).
体外研究	Reparixin is a potent functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively). Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2.
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纯度及产品资料	98%

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