gs

GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。

GS-9901 是一种具有选择性、口服活性和高效性的 PI3Kδ 抑制剂（IC50：1 nM），可用于研究非霍奇金淋巴瘤和慢性淋巴细胞白血病。

GS-9191是一种DNA 聚合酶α和ß 的强效抑制剂 ，是一种新型核苷类似物9-(2-膦酰甲氧基乙基)鸟嘌呤(PMEG)的原药 ，可渗透皮肤并在上皮层代谢为活性核苷三磷酸类似物。GS-9191具有抗增殖活性，以剂量相关的方式减少乳头瘤的大小。GS-9191可能对治疗HPV 引起的病变有作用。

GS-9667是一种A（1）腺苷受体（AR）的选择性部分激动剂，通过降低游离脂肪酸（FFA）可有效治疗2型糖尿病（T2DM）和血脂异常。

GS-6620 PM 是GS-6620的衍生物。GS-6620是一种口服的抗丙型肝炎病毒聚合酶抑制剂，是一种新型强效的C-核苷腺嘌呤类似物单磷酸酯原药。GS-6620对其他病毒的活性有限，对密切相关的牛病毒性腹泻病毒仅保持部分活性（EC50，1.5μM）。

GS-829845 是一种 JAK1 抑制剂，是 Filgotinib 活性代谢物的主要成分，其效力比母体低约 10 倍且半衰期更长。

GS87 是 GSK3（糖原合酶激酶 3）的高度特异性抑制剂，可诱导 AML 细胞的广泛分化。

GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).

GS-566500 is a compound of Sofosbuvir metabolite.

GS-2278是一种高效的LPAR1 (溶血磷脂酸受体 1) 拮抗剂，预期可应用于特发性肺纤维化 (IPF) 的研究。

GS967 是一种有效的、选择性的心脏晚期钠电流（late I Na）抑制剂，心室肌细胞和心脏中的IC50分别为0.13和0.21 μM。

GS 39783 是 GABABR 的正变构调节剂 (PAM)，可降低酒精的动机特性,减少精神兴奋剂的条件强化和条件性奖励。

GS-9148 is a dAMP analog. It also maintains its antiviral activity against drug-resistant HIV.

GS-143 是选择性的IκBα泛素化抑制剂，抑制 SCFβTrCP1介导的IκBα泛素化作用，IC50=5.2 μM。GS143 抑制NF-κB 的活化和靶基因的转录，并且不抑制蛋白酶体的特性，并具有抗哮喘作用。

GS 283 is a Ca(2+) antagonist. GS 283 is also a weak histamine and muscarinic receptor blocker in rat and guinea pig tracheal smooth muscles.

GS 389 is a novel tetrahydroisoquinoline analog with vasorelaxant properties. GS-389 significantly inhibited cGMP phosphodiesterase from the rabbit brain and increased cGMP levels in the rat aorta.

GS-462808 is a late sodium current inhibitor of the cardiac Nav1.5 channel. GS-462808 had lower brain penetration and serendipitously lower activity at the brain isoforms.

GS-6620 is a HCV nonstructural protein 5B (NS5B) inhibitor.

GS-9851, a HCV nonstructural protein 5B (NS5B) inhibitor, is used potentially for the treatment of HCV infection.

GS-7339 is a bioactive chemical.

GS-7339 monofumarate is a bioactive chemical.

GS-441524tris-isobutyryl ester is a prodrug form of the antiviral nucleoside analog and remdesivir metabolite GS-441524 .1It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells with an EC50value of 0.26 μM. 1.Mackman, R.L., Hui, H.C., Perron, M., et al.Prodrugs of a 1’-CN-4-aza-7,9-dideazaadenosine C-nucleoside leading to the discovery of remdesivir (GS-5734) as a potent inhibitor of respiratory syncytial virus with efficacy in the african green monkey model of RSVJ. Med. Chem.64(8)5001-5017(2021)

GS-704277, an alanine metabolite derived from Remdesivir, a nucleoside analogue acknowledged for its potent antiviral efficacy, demonstrates remarkable effectiveness in vitro for the management of SARS-CoV-2 (COVID-19) infection[1][2].

GS-493, a highly specific protein tyrosine phosphatase SHP2 (PTPN11) inhibitor, exhibits remarkable potency with an IC50 of 71 nM. It displays 29- and 45-fold greater affinity towards SHP2 compared to its related counterparts, SHP1 and PTP1B, respectively. In addition, GS-493 impedes both cellular motility and growth of cancer cells, portraying promising antitumor effects.