GSK484 HCl

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Chemical Structure| 1652591-81-5 同义名 : GSK484 (hydrochloride);GSK484 hydrochloride
CAS号 : 1652591-81-5
货号 : A268467
分子式 : C27H32ClN5O3
纯度 : 99%+
分子量 : 510.028
MDL号 : MFCD30343874
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(235.28 mM)，配合低频超声助溶，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

H2O: 50 mg/mL(98.03 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 GSK484 HCl exhibits strong affinity for PAD4 in its low-calcium state, with IC50s of 50 nM without calcium and 250 nM with 2 mM calcium. It also concentration-dependently inhibits PAD4's citrullination of the BAEE substrate in the presence of 0.2 mM calcium, as shown by an ammonia release assay[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.80mL

1.96mL

0.98mL

19.61mL

3.92mL

1.96mL
参考文献

[1]Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

[2]Cedervall J, et al. Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice. Oncoimmunology. 2017 Apr 20;6(8):e1320009.