drug-related

SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂，Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂，可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。

(Z)-2-fluoro-1,3-bis(4-methoxyphenyl)prop-2-en-1-one 是一种筛选化合物，可用于新药研发相关研究。

Terpin hydrate 是一种祛痰药，可除去急慢性支气管炎病人的黏液。

Lopinavir (ABT-378) 是一种选择性肽模拟 HIV-1 蛋白酶的高效抑制剂。它通过阻止 HIV-1 的成熟而起作用，从而阻断其感染性。它也是 SARS-CoV 3CLpro 的抑制剂。

Rabeprazole Sulfide (Rabeprazole Related Compound E) 是 Rabeprazole 的活性代谢产物。Rabeprazole 是一种质子泵抑制剂类的抗溃疡药物，有效抑制幽门螺旋杆菌的活性，可通过与胃壁细胞中的(H+ K+)-ATPase 相互作用来抑制胃酸分泌，可研究各种消化系统疾病。

Buparvaquone (BW 720C) 是与parvaquone 和atovaquone 有关的一种羟基萘醌类抗原虫药。

Drotaverine hydrochloride 是磷酸二酯酶 4 (PDE4)的抑制剂，也是 L 型电压依赖钙通道(L-VDCC)的阻滞剂，可阻断3',5'-环腺苷单磷酸的降解。它在体内有抗痉挛效果，但无抗胆碱能的效果。

Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

Izeltabart Tapatansine (IMGC-936) 是 CHO 表达的人源化靶向 ADAM9 表达肿瘤的基于美登素的 ADC 化合物，对 ADAM9 阳性人肿瘤细胞系表现出细胞毒性，可用于研究癌症。

Pramiracetam (CI-879) 来源于piracetam，能改善脑外伤引起的认知障碍。它是更有效的促智药物。

AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens. IC50 value: 2-4 ug ml (MICs) Target: antibacterial agent AVX13616 was as active as mupirocin i

CL-A3-7 作为一种病毒-细胞融合抑制剂，专门针对RSVF蛋白，通过阻止病毒和宿主细胞IGF1R之间的交互作用来发挥效能。该化合物不仅能有效地阻断野生型RSV的感染，还对K394R变异株也有显著的抑制作用，因此极具潜力用于开发抗RSV药物及进行耐药性的研究。

PAMAM Dendrimer G0.0 amine 是一种孔形成通道拮抗剂，对炭疽毒素保护抗原 63 (PA63, IC50为 231 nM) 和肉毒梭菌 C2 毒素亚基 (C2IIa, IC50为 940 nM) 有效。在浓度为 10 和 20 µM 时，能够减少 C2 毒素引起的 HeLa 细胞死亡。此外，它作为镍的螯合剂，并在与聚砜膜结合的壳聚糖复合物中，能选择性地捕捉并储存二氧化碳 (CO2) 用于气体进料系统中。PAMAM Dendrimer G0.0 amine 已用于合成 PAMAM Dendrimer G0.5 Carboxylate (CAS 339334-01-9) 和 PAMAM Dendrimer G1.0 Amine (CAS 142986-44-5)。此化合物用于研究感染、癌症和药物递送系统。

AcBut-N-Ac-γ-Calicheamicin 是一种 ADC 毒素，通过引发 DNA 双链断裂导致细胞周期停滞和凋亡 (Apoptosis)。其主要用于抗体药物偶联物 (ADC) 的合成，有潜力应用于癌症研究，特别是急性淋巴细胞白血病 (ALL) 和其他血液系统恶性肿瘤的研究。

AK-968-11563024 是一种作用于海洋V. vulnificus NAT [(VIBVN)NAT] 的抑制剂，具有18.86 µM的IC50。海洋V. vulnificus中的NAT（芳香胺 N-乙酰转移酶）在药物代谢中扮演着重要角色，并促进药物耐受性的形成。因此，AK-968-11563024 可用于与药物耐受性相关的研究。

DSPE-PEG-OH (MW 4000) 是一种羟基封端的PEG化磷脂，具有疏水尾部，允许封装和聚集其他疏水药物，羟基末端可以进一步反应。DSPE-PEG-OH (MW 4000) 常用于脂质体或脂质纳米颗粒的制备，适用于药物递送和增强药物吸收的研究。

C-lock-G5-DUO-5 是一种 Drug-linker，DUO-5是一种微管抑制剂，具有抗癌活性，与 C-lock-G5 采用稳定共价不可逆连接方式,重新引入共价键联接，更好的稳定性,改进的 PK 特性。可用于 BA1301等相关产品的制备与合成。

Loxapine 是 D2DR 和 D4DR 抑制剂和5-羟色胺能受体拮抗剂，是一种抗精神病药物，主要用于治疗精神分裂症。

(R)-Licarbazepine Acetate is a hopeful antiepileptic drug structurally related to Carbamazepine and Oxcarbazepine.

L-Ibotenic acid is a chemical compound and psychoactive drug which occurs naturally in Amanita muscaria and related species of mushrooms typically found in the temperate and boreal regions of the northern hemisphere. It is a conformationally-restricted an

Diethylhomospermine is a drug potentially for the treatment of AIDS-related chronic diarrhea.Diethylhomospermine also shows promising anticancer activity.

Difenamizole is a nonsteroidal anti-inflammatory drug (NSAID), which is a pyrazolinone analgesic drug-related to Analgin. It has monoaminergic properties, including inhibition of monoamine oxidase, an increase of pargyline-induced striatal dopamine levels

Phenindamine Tartrate is an antihistamine and anticholinergic drug closely related to cyproheptadine. It is used to treat symptoms of the common cold and allergies, such as sneezing, itching, rashes, and hives.

Ensartinib (X-396) is a potent and dual ALK MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1]. The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.