Reparixin L-lysine salt
作者：齊岳
發(fā)布時(shí)間：2023-09-12
09:12:38
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Reparixin L-lysine salt
產(chǎn)品描述：
| 產(chǎn)品描述 | Reparixin L-lysine salt is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor. |
| 靶點(diǎn)活性 | CXCR1:1 nM (in cells), CXCR1:5.6 nM (CXCR1wt, in L1.2 cells), CXCR1:80 nM (CXCR1Ile43Val; in L1.2 cells), CXCR2:100 nM (in cells) |
| 體外活性 | Reparixin is a potent CXCL8-induced inhibitor 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.Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2]. 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)[1]. |
| 體內(nèi)活性 | The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [14C]-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)[3]. |
| 別名 | Repertaxin L-lysine salt, REPERTAXIN L-賴氨酸鹽 |
| 分子量 | 429.57 |
| 分子式 | C20H35N3O5S |
| CAS No. | 266359-93-7 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 99 mg/mL (230.46 mM),Need ultrasonic
DMSO: 99 mg/mL (230.46 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯(lián)系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
主營(yíng)產(chǎn)品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉(zhuǎn)換、石墨烯、光電材料、點(diǎn)擊化學(xué)、凝集素、載玻片、蛋白質(zhì)交聯(lián)劑、脂質(zhì)體、蛋白、多肽、氨基酸、糖化學(xué)等。
