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GLPG1837 {[allProObj[0].p_purity_real_show]}

货号：A647373 同义名： ABBV-974

GLPG-1837 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator1, shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor.

GLPG1837 化学结构 CAS号：1654725-02-6
GLPG1837 化学结构
CAS号：1654725-02-6
GLPG1837 3D分子结构
CAS号：1654725-02-6
GLPG1837 化学结构 CAS号：1654725-02-6
GLPG1837 3D分子结构 CAS号：1654725-02-6
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GLPG1837 纯度/质量文件 产品仅供科研

货号：A647373 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 CFTR ↓ 其他靶点 纯度
Ataluren ✔ 98%
Lumacaftor ++++

F508del-CFTR, EC50: 0.1 μM

 		98%
CFTR(inh)-172 +++

CFTR, Ki: 300 nM

 		99%+
GlyH-101 +

CFTR, Ki: 4.3 μM

 		99%+
IOWH-032 ++

CFTR, IC50: 1.01 μM

 		99%+
Tezacaftor ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GLPG1837 生物活性

描述 Cystic fibrosis (CF) is the most common life-threatening autosomal recessive disorder in Caucasian populations. It is caused by mutations of the gene for the cystic fibrosis transmembrane conductance regulator (CFTR) protein. The most common mutation, F508del, belongs to the class II trafficking defects, where folding of the CFTR protein is impaired, resulting in a reduction of the amount of ion channel present on the cell surface. With the G551D mutation (class III), the amount of protein is not affected but its open probability is reduced, resulting as well in a reduced channel gating[2]. GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively[2]. GLPG1837 had an attractive in vitro ADME (ADME: absorption, distribution, metabolism, excretion) profile, showing low Clint, unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel[2]. GLPG1837 is reversible CFTR potentiator, with an apparent affinity within a range of 0.2 ∼ 2 µM[3]. The pharmacokinetic profile of GLPG1837 was attractive, showing a low Cl, unb and good F% in both rat and dog. In rats and dogs, the clearance rate (CL) of 1 mg/kg GLPG1837 was 1.92 and 0.32 L/h/kg, respectively. In addition, T1/2 was 1.84 hours in rats while 3 hours in dogs. The oral bioavailability of GLPG1837 was 67% in rats and more than 100% in dogs with oral administration of 5 mg/kg[2].

GLPG1837 动物研究

Dose Rat: 5 mg/kg[1] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[1] Dogs[1]
Dose 1 mg/kg (i.v.)
5 mg/kg (p.o.) 		1 mg/kg (i.v.)
5 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o.
F 0.67 > 100%
Vd 4.8 L/kg 1.4 L/kg
T1/2 1.84 h 3.0 h
CL 1.92 L/h/kg 0.32 L/h/kg
CLunb 24 L/h/kg 6.4 L/h/kg

GLPG1837 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
NCT02325037 Healthy Phase 1 Completed - Belgium ... 展开 >> SGS LSS Clinical Pharmacology Unit Antwerp Antwerp, Belgium 收起 <<
NCT02562950 Healthy Phase 1 Completed - Belgium ... 展开 >> SGS LSS Clinical Pharmacology Unit Antwerp Antwerp, Belgium 收起 <<
NCT02707562 Cystic Fibrosis Phase 2 Completed - Australia ... 展开 >> Royal Adelaide Hospital Adelaide, Australia The Prince Charles Hospital Chermside, Australia Monash Medical Centre Clayton, Australia Sir Charles Gairdner Hospital Nedlands, Australia Mater Adult Hospital South Brisbane, Australia Czech Republic Fakultni nemocnice v Motole Praha 5, Czech Republic Germany Charité Universitätsmedizin Berlin Berlin, Germany Universitätsklinkikum Koeln Cologne, Germany Uniklinik Carl-Gustav-Carus Dresden, Germany Lungenheilkunde München-Pasing München, Germany Ireland Beamont Hospital Dublin, Ireland St. Vincent's University Hospital Dublin, Ireland United Kingdom Queen Elizabeth University Hospital Glasgow, United Kingdom Liverpool Heart and Chest Hospital Liverpool, United Kingdom Royal Brompton Hospital London, United Kingdom The Medicines Evaluation Unit Ltd Manchester, United Kingdom 收起 <<

GLPG1837 参考文献

[1]Van der Plas SE, Kelgtermans H, et al. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent. J Med Chem. 2018 Feb 22;61(4):1425-1435.

[2]Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent. J Med Chem. 2018 Feb 22;61(4):1425-1435. doi: 10.1021/acs.jmedchem.7b01288. Epub 2018 Jan 10. PMID: 29148763.

[3]Yeh HI, Sohma Y, Conrath K, Hwang TC. A common mechanism for CFTR potentiators. J Gen Physiol. 2017 Dec 4;149(12):1105-1118. doi: 10.1085/jgp.201711886. Epub 2017 Oct 27. PMID: 29079713; PMCID: PMC5715911.

GLPG1837 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.70mL

5.74mL

2.87mL

GLPG1837 技术信息

CAS号1654725-02-6
分子式C16H20N4O3S
分子量 348.42
别名 ABBV-974
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 250 mg/mL(717.52 mM)，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
动物实验配方

Tags: GLPG1837 | 1654725-02-6 | ABBV-974 | GLPG 1837 | GLPG-1837 | ABBV974 | ABBV 974 | CFTR Agonist | Membrane Transporter/Ion Channel | Autophagy | CFTR | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GLPG1837 纯度/质量文件 | GLPG1837 亚型比较 | GLPG1837 生物活性 | GLPG1837 动物研究 | GLPG1837 临床数据 | GLPG1837 参考文献 | GLPG1837 实验方案 | GLPG1837 技术信息

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