GSK484 HCl
GSK484 is a potent PAD-4 inhibitor (Protein-arginine deiminase type-4). GSK484 potently binds to the low-calcium form of PAD4 in a reversible manner (IC50 of 50 nM) and appears to be competitive with substrate. GSK484’s selectivity for PAD4 over PAD1-3 was shown in cells and also confirmed with recombinant enzymes. This probe is an inhibitor of cellular citrullination in primary neutrophils, and further phenotypic profiling has confirmed its ability to inhibit NET formation in both mouse and human neutrophils. GSK484 exhibits favourable pharmacokinetic profiles, with low-moderate clearance, and good volume of distribution and half-life in mouse and rat, and has suitable a PK profile for use as a potential in vivo tool. (http://www.thesgc.org/chemical-probes/GSK484).
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化学信息
| 名称 | GSK484 HCl |
|---|---|
| Iupac 化学名称 | ((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride |
| 同义词 | GSK484; GSK-484; GSK 484. |
| 英文同义词 | GSK484; GSK-484; GSK 484. |
| 分子式 | C27H32ClN5O3 |
| 分子量 | 510.035 |
| Smile | O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3N(C)C(C(N4CC5CC5)=CC6=C4C=CC=C6)=NC3=C2.[H]Cl |
| InChiKey | MULKOGJHUZTANI-ADMBKAPUSA-N |
| InChi | InChI=1S/C27H31N5O3.ClH/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16;/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3;1H/t19-,23+;/m0./s1 |
| Cas号 | 1652591-81-5 |
| 相关CAS号 |
订购信息
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