瑞帕利辛L-赖氨酸盐 - CAS:266359-93-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	瑞帕利辛L-赖氨酸盐
英文名称:	Reparixin L-lysine salt
别名:	REPERTAXIN L-赖氨酸盐;Repertaxin L-赖氨酸盐 Repertaxin L-lysine salt
CAS No:	266359-93-7	分子式:	C₂₀H₃₅N₃O₅S	分子量:	429.57
CAS No:	266359-93-7
分子式:	C₂₀H₃₅N₃O₅S
分子量:	429.57

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R10319 瑞帕利辛L-赖氨酸盐 ≥98% (psaitong)

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包装规格：

5mg in glass bottle

溶解性：

溶于水（100 mg/mL 超声），溶于DMSO（100 mg/mL 超声）

产品描述：

基本信息

产品编号：	R10319
产品名称：	Reparixin L-lysine salt
CAS:	266359-93-7	储存条件	粉末	-20℃	四年

分子式：	C20H35N3O5S		溶于液体	-80℃	6个月
分子量：	429.57			-20℃	1个月
化学名：	(2S)-2,6-diaminohexanoic acid;(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.3279mL	11.6395mL	23.2791mL
5mM	0.4656mL	2.3279mL	4.6558mL
10mM	0.2328mL	1.1640mL	2.3279mL

生物活性

产品描述	一种趋化因子受体1/2 (CXCR1/2)活化的变构抑制剂。
靶点	CXCR
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 5.6nM and 80nM 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.
体内研究	The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [14 C]-Reparixin L-lysine salt.Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50µg/mL,but lower at higher concentrations.Although radioactivity is rapidly distributed into rat tissues,Vss is low (about 0.15L/kg) in both rat and dog.Nevertheless,Reparixin is more rapidly eliminated in rats (t1/2~0.5h) than in dogs (t1/2~10h).

推荐实验方法(仅供参考)

细胞实验:

L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37℃ for 15 min in the presence of vehicle or of Reparixin (1nM-1μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber.Different agonists are seeded in the lower compartment of the chamber at the following concentrations:1nM CXCL8,0.03nM fMLP,10nM CXCL1,2.5nM CCL2,30nM C5a.The chemotactic chamber is incubated at 37℃ in air with 5% CO2 for 45 min (human PMNs) or 2h (monocytes).At the end of incubation,the filter is removed,fixed,and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding.L1.2 migration is evaluated using 5μm pore size Transwell filters.

动物实验:

Rats and Dogs

Male and female Sprague-Dawley CD (albino) rats and male Lister Hooded (partially pigmented) rats are used.Male and female beagle Dogs (age about 15 months,bodyweight range 8.3-9.4kg at the time of dosing) are used.Rats and Dogs are dosed i.v.with repurified [14C]-Reparixin free acid and an equivalent quantity of L-lysine suitably radiodiluted with Reparixin L-lysine salt in a solution of sterile isotonic (0.9%,w/v) saline. Rats are dosed with a solution of total drug concentration 9mg/mL at a dose volume of 5mL/kg (30mg free Reparixin /kg) by bolus injection into a caudal vein.Dogs are dosed with a solution of total drug concentration 100mg/mL at a dose volume of 0.5mL/kg (33mg free Reparixin/kg) by bolus injection into a superficial forelimb vein.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果