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CAS No.: 954126-98-8

Danirixin/达尼利星 Catalog No. CSN18630

Synonyms: GSK1325756;Danirixin IV

Danirixin is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

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生物活性

实验方案

技术信息

生物活性

描述The CXC chemokine receptor 2 (CXCR2) mediates chemotaxis of leukocytes and controls the extravasation and activation of neutrophils. Danirixin is a small-molecule, selective, and reversible CXCR2 antagonist^[2]. Danirixin competes with CXCL8 binding to the membranes prepared from Chinese hamster ovary cells transfected with human CXCR2 or CXCR1 with IC50 values of 12.5nM (pIC50 = 7.90 ± 0.04) and 977nM (pIC50 = 6.03 ± 0.05), respectively. It also acts as a competitive antagonist against CXCL8 in Ca²⁺ mobilization assays with a Kb of 6.5nM and a pA₂ of 8.44. Oral administration of Lewis rats with danirixin at doses of 0.3, 3, and 30mg/kg increased the EC50 value for CXCL2-induced CD11b expression in neutrophils from 4.5nM (the vehicle-treated group) to 9.4, 11.9, and 38.1nM, respectively. In fasted rats following inhaled lipopolysaccharide challenge, danirixin at a dosage of 10 mg/kg led to 84% inhibition of neutrophil influx to the lung with an ED50 value of 1.4mg/kg. In fed rats, 10mg/kg of danirixin resulted in 64% inhibition with an ED50 value of 2.3 mg/kg. Danirixin also dose-dependently inhibited neutrophils when administered to fasted rats 1 hour prior to ozone exposure with an ED50 value of 16.0 mg/kg^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03136380	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 1	Completed	-	Japan ... more >> GSK Investigational Site Tokyo, Japan, 162-0053 Collapse <<
NCT02469298	Virus Diseases	Phase 2	Completed	-	-
NCT02469298	-	-	Completed	-	-

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参考文献

[1] Busch-Petersen J, Carpenter DC, et al. Danirixin: A Reversible and Selective Antagonist of the CXC Chemokine Receptor 2. J Pharmacol Exp Ther. 2017 Aug;362(2):338-346.
[2] Miller BE, Mistry S, Smart K, et al. The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects. BMC Pharmacol Toxicol. 2015;16:18.
[3] Busch-Petersen J, Carpenter DC, Burman M, et al. Danirixin: A Reversible and Selective Antagonist of the CXC Chemokine Receptor 2. J Pharmacol Exp Ther. 2017;362(2):338-346.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2629 mL
- 11.3147 mL
- 22.6293 mL
- 5 mM
- 0.4526 mL
- 2.2629 mL
- 4.5259 mL
- 10 mM
- 0.2263 mL
- 1.1315 mL
- 2.2629 mL

技术信息

CAS号

954126-98-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21ClFN3O4S

运输

蓝冰

分子量

441.90

别名

GSK1325756;Danirixin IV

溶解度

DMSO	87.0 mg/mL (196.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03136380	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 1	Completed	-	Japan ... more >> GSK Investigational Site Tokyo, Japan, 162-0053 Collapse <<
NCT02469298	Virus Diseases	Phase 2	Completed	-	-
NCT02469298	-	-	Completed	-	-
NCT03457727	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 1	Completed	-	United States, Kansas ... more >> GSK Investigational Site Overland Park, Kansas, United States, 66211 Collapse <<
NCT02927431	-	-	Terminated(The study was stopp... more >>ed early due to lack of enrollment.) Collapse <<	-	-
NCT02201303	Infections, Respiratory Syncyt... more >>ial Virus Collapse <<	Phase 1	Completed	-	United States, New York ... more >> GSK Investigational Site Syracuse, New York, United States, 13210 Collapse <<
NCT02927431	Virus Diseases	Phase 2	Terminated(The study was stopp... more >>ed early due to lack of enrollment.) Collapse <<	-	-
NCT03250689	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Active, not recruiting	December 3, 2018	United Kingdom ... more >> GSK Investigational Site Dundee, United Kingdom, DD1 9SY Collapse <<
NCT03034967	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	-
NCT03170232	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Recruiting	March 31, 2020	United States, Alabama ... more >> GSK Investigational Site Recruiting Birmingham, Alabama, United States, 35294 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, California GSK Investigational Site Recruiting San Diego, California, United States, 92103-8415 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Torrance, California, United States, 90502 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Colorado GSK Investigational Site Recruiting Denver, Colorado, United States, 80206 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Iowa GSK Investigational Site Recruiting Iowa City, Iowa, United States, 52243 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Maryland GSK Investigational Site Recruiting Baltimore, Maryland, United States, 21224 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Michigan GSK Investigational Site Recruiting Ann Arbor, Michigan, United States, 48109-5360 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Minnesota GSK Investigational Site Recruiting Saint Paul, Minnesota, United States, 55130 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Pennsylvania GSK Investigational Site Recruiting Philadelphia, Pennsylvania, United States, 19140 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Recruiting Pittsburgh, Pennsylvania, United States, 15213 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com United States, Texas GSK Investigational Site Recruiting Houston, Texas, United States, 77030 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com GSK Investigational Site Not yet recruiting San Antonio, Texas, United States, 78229 Contact: US GSK Clinical Trials Call Center 877-379-3718 GSKClinicalSupportHD@gsk.com Contact: EU GSK Clinical Trials Call Center +44 (0) 20 8990 4466 GSKClinicalSupportHD@gsk.com Collapse <<
NCT02453022	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 1	Completed	-	United States, Kansas ... more >> GSK Investigational Site Overland Park, Kansas, United States, 66211 Collapse <<
NCT02130193	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> GSK Investigational Site Birmingham, Alabama, United States, 35294 United States, Colorado GSK Investigational Site Denver, Colorado, United States, 80206 United States, Iowa GSK Investigational Site Iowa City, Iowa, United States, 52242 United States, Pennsylvania GSK Investigational Site Oaks, Pennsylvania, United States, 19456 GSK Investigational Site Philadelphia, Pennsylvania, United States, 19140 United States, South Carolina GSK Investigational Site Spartanburg, South Carolina, United States, 29303 Germany GSK Investigational Site Frankfurt, Hessen, Germany, 60596 GSK Investigational Site Neu isenburg, Hessen, Germany, 63263 GSK Investigational Site Dueren, Nordrhein-Westfalen, Germany, 52349 GSK Investigational Site Essen, Nordrhein-Westfalen, Germany, 45359 GSK Investigational Site Magdeburg, Sachsen-Anhalt, Germany, 39112 GSK Investigational Site Leipzig, Sachsen, Germany, 04207 GSK Investigational Site Leipzig, Sachsen, Germany, 04275 GSK Investigational Site Grosshansdorf, Schleswig-Holstein, Germany, 22927 GSK Investigational Site Berlin, Germany, 10787 GSK Investigational Site Berlin, Germany, 10789 Collapse <<
NCT02130193	-	-	Completed	-	-

Danirixin/达尼利星 Catalog No. CSN18630

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