mk 8

MK8722 是一种全身性泛 AMPK 激活剂。

MK-8353 (SCH900353) 是口服有效的ERK1 2选择性抑制剂，IC50分别为 23.0 nM 和 8.8 nM。它显示出抗肿瘤活性。

MK-8325是一种有效且可口服的HCV NS5A 抑制剂，对多种基因型具有复制活性。MK-8325在体外和体内试验显示生物利用度且具有良好的总体ADME 特征。

MK-8033 hydrochloride 是一种有效的、具有口服活性的 ATP 竞争性 c-Met Ron 双重抑制剂 ，对c-Met 的为1 nM ，对Ron 的IC50为7nM。MK-8033 hydrochloride 对活化的激酶构象 (activated kinase conformation)具有很高的亲和力，可用于乳腺癌，膀胱癌、非小细胞肺癌 (NSCLC)等癌症的研究。

Lovastatin (MK-803) 是一种 HMG-CoA 还原酶抑制剂 (IC50=3.4 nM)。Lovastatin 可以降低胆固醇，常用作降血脂剂，用于治疗高胆固醇血症。

MK-8189是一种高效和选择性的嘧啶类PDE10A抑制剂，Ki = 0.029nM，具有优异的PDE（磷酸二酯酶）选择性，可用于治疗精神分裂症。

MK-8719 是高效的O-GlcNAcase 选择性抑制剂 (hOGA 的Ki=为 7.9 nM)，中枢神经系统渗透性能良好。

Dizocilpine (MK-801) 是一种选择性非竞争性NMDA 受体拮抗剂，Kd=37.2 nM，是一种抗惊厥剂。它通过与 NMDA 相关离子通道内的一个位点结合而起作用，从而阻止 Ca2+的流动。

MK-886 (L 663536)是一种细胞可渗透的，具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂，可以诱导细胞凋亡。

Birabresib (MK-8628) 是一种 BRD2 3 4抑制剂，IC50值为 92 到 112 nM 之间，具有潜在的抗肿瘤活性。

SCH900776 (MK-8776) 是一种靶向细胞周期检查点激酶 1(Chk1) 的抑制剂，IC50值为 3 nM。它比对 CDK2 和 Chk2 的选择性分别高 50 和 500 倍，具有潜在的放射增敏和化学增敏活性。

MK-8245 analog 是 MK-8245 的类似物，MK-8245 是一种肝脏靶向的硬脂酰辅酶 A 去饱和酶 (SCD) 抑制剂。它可用于治疗血脂异常和糖尿病。

MK8745是一种极光激酶抑制剂，IC50值为0.6 nM。

MK-8998 是一种T型钙通道拮抗剂，可能用于治疗精神分裂症。然而，在治疗急性精神病住院患者方面，根据第四周的PANSS评分，MK-8998未显示出有效性。

Caged MK801 (cMK801) 是一种选择性的、非竞争性的、不可逆的 NMDA 受体开放通道阻断剂。其 NVOC 笼结构在神经药理学上相容，不会影响分子的本身活性。

MK-8457是一种SYK ZAP70双重抑制剂，可用于类风湿关节炎的研究。

MK-8970 is an acetal carbonate prodrug of raltegravir with enhanced colonic absorption.

MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂，对于PHD2的IC50=1 nM。

MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay. in vivo: Administration of MK-8245 at 10 mg kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg kg.

MK-8876 is an Inhibitor of HCV NS5B Site D.

IDN-1965 is a potent, broad-spectrum, irreversible caspase inhibitor. IDN-1965 is markedly effective at inhibiting Fas-mediated apoptosis by multiple routes of administration. The therapeutic potential of caspase inhibitors appears promising for the treatment of apoptosis-mediated liver injury based on potency and postinsult efficacy.

MK-8718 is an HIV protease inhibitor with a selective orally bioavailable inhibitor with good pharmacokinetic characteristics.

Alinastine is a noncompetitive histamine H1 receptor antagonist.

MK-8825 is a CGRP receptor antagonist.