GLPG2938
目录号 : GC62990
An S1P2 antagonist
Cas No.:2130996-00-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GLPG2938 is sphingosine-1-phosphate receptor 2 (S1P2) antagonist.1 It inhibits S1P-induced calcium flux in CHO cells overexpressing human S1P2 (IC50 = 8.8 nM). GLPG2938 inhibits S1P-induced IL-8 release in HFL1 cells (IC50 = 0.6 nM) and S1P-induced contraction of human lung fibroblasts. In vivo, GLPG2938 (3, 10, and 30 mg/kg) prevents epithelial damage and pulmonary fibrosis, structural distortion, and inflammation in a mouse model of bleomycin-induced pulmonary fibrosis.
1.Mammoliti, O., Palisse, A., Joannesse, C., et al.Discovery of the S1P2 antagonist GLPG2938 (1-[2-ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a preclinical candidate for the treatment of idiopathic pulmonary fibrosisJ. Med. Chem.64(9)6037-6058(2021)
| Cas No. | 2130996-00-6 | SDF | |
| 分子式 | C20H19F6N7O2 | 分子量 | 503.4 |
| 溶解度 | DMSO : 100 mg/mL (198.65 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9865 mL | 9.9325 mL | 19.8649 mL |
| 5 mM | 0.3973 mL | 1.9865 mL | 3.973 mL |
| 10 mM | 0.1986 mL | 0.9932 mL | 1.9865 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis
J Med Chem 2021 May 13;64(9):6037-6058.PMID:33939425DOI:10.1021/acs.jmedchem.1c00138
Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling could be effective for the treatment of idiopathic pulmonary fibrosis (IPF). However, only a few antagonists have been so far disclosed. A chemical enablement strategy led to the discovery of a pyridine series with good antagonist activity. A pyridazine series with improved lipophilic efficiency and with no CYP inhibition liability was identified by scaffold hopping. Further optimization led to the discovery of 40 (GLPG2938), a compound with exquisite potency on a phenotypic IL8 release assay, good pharmacokinetics, and good activity in a bleomycin-induced model of pulmonary fibrosis.