{{cart_num}}
My CartCAS：1206161-97-8
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
Qty：
Size：
| CAS | 1206161-97-8 |
| Name | GLPG0634 |
| Molecular Formula | C21H23N5O3S |
| Molecular Weight | 425.5 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD20527867 |
| SMILES | O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2 |
| InChIKey | RIJLVEAXPNLDTC-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27) |
| PubChem CID | 49831257 |
| Target Point | JAK |
| Passage | JAK/STAT Signaling |
| Background | GLPG0634 is a selective JAK inhibitor. |
| Biological Activity | GLPG0634 是一种选择性的 JAK 抑制剂，能够有效抑制 JAK1，JAK2，JAK3 和 TYK2 的活性，IC50 值分别为 10 nM，28 nM，810 nM 和 116 nM[1-2]。 |
| IC50 | JAK1:10nM;JAK2:28nM;JAK3:810nM;Tyk2:116nM [1-2] |
| In Vitro | GLPG0634不抑制由EPO或PRL诱导的JAK2同二聚体介导的信号传导(IC50>10μM)[2]。GLPG0634剂量依赖性地抑制由IL-4介导的Th2细胞的分化，IL-4是通过JAK1和JAK3发出信号的细胞因子。 GLPG0634还以1μM或更低的相似效力抑制Th1分化[1]。 |
| In Vivo | GLPG0634(3，10，30mg/kg，口服)剂量依赖性地预防治疗性大鼠CIA模型中的疾病进展。 GLPG0634(50 mg/kg，op)保护骨骼和软骨免于降解，有效减少爪子中T细胞(CD3 +细胞)和巨噬细胞(F4/80 +细胞)的浸润，并降低测量的所有细胞因子和趋化因子的血清水平，包括IL-6，IP-10，XCL1和MCP-1 [1]。 GLPG0634(0.1和0.3mg/kg)在大鼠CIA模型中显示出功效[2]。 |
| Animal Experiment | GLPG0634以5mg/kg(剂量体积为5mL/kg)口服给药为单次食道管饲，并通过尾静脉以1mg/kg(剂量体积为5mL/kg)静脉内给药。在大鼠研究中，每组由三只大鼠组成，并通过颈静脉收集血液样品。在小鼠研究中，每组由21只小鼠(n = 3 /时间点)组成，并且在异氟烷麻醉下通过心内穿刺收集血液样品。肝素锂用作抗凝剂，血液在0.05，0.25，0.5，1，3，5和8小时(静脉注射)和0.25，0.5，1，3，5，8和24小时(口服)。 |
| Kinase Experiment | 重组JAK1，TYK2，JAK2和JAK3用于在50mM HEPES(pH 7.5)，1mM EGTA，10mM MgCl 2，2mM DTT和0.01％吐温20中开发活性测定.JAK蛋白的量根据每个测定。等分试样，随时间保持初始速度和线性。 ATP浓度相当于实验Km值的4倍，底物浓度(ULight-缀合的JAK-1(Tyr1023)肽)对应于实验测定的Km值。在室温(RT)温育90分钟后，通过在Lance检测缓冲液中加入2nM铕 - 抗磷酸酪氨酸Ab和10mM EDTA来测量磷酸化底物的量。在加入ATP之前，通过在室温下将化合物与化合物预孵育60分钟来测定化合物IC 50值。 |
| Data Literature Source | [1]. Van Rompaey L，et al. Preclinical characterization of GLPG0634，a selective inhibitor of JAK1，for the treatment of inflammatory diseases. J Immunol. 2013，191(7)，3568-3577. [2]. Menet CJ，et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17 |
| Unit | Piece |
| Specification | 5mg 10mg |
GLPG0634 是一种选择性的 JAK 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
