tetrazole

Tetrazole (1H-TETRAZOLE) 是羧酸的生物等排体，具有相当的抗菌性能。

Mephetyl tetrazole 是一种作用于钾离子通道 (potassium channel) Kv1.5 的阻断剂，其 IC50 值为 330 nM，可应用于癌症研究。

Bentemazole曾被研究用作抗真菌化合物。

Penicillamine (Artamine) 是一种 penicillin 的代谢降解产物，是一种螯合剂，可作用于威尔逊氏病。

Pentetrazol 是一种 GABA(A) 受体拮抗剂，具有中枢神经系统和呼吸兴奋剂的活性。

Valsartan (CGP 48933) 是一种血管紧张素 II 受体拮抗剂，有用于高血压和心力衰竭的研究潜力。

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.

CB 168是有效的靶向异亮基 tRNA 合成酶 (IleRS) 选择性氨基酰基氨基酰芳基四唑抑制剂。

Antifungal agent 52 (compound 6c) 是四唑衍生物。Antifungal agent 52 抑制麦角固醇 的合成。Antifungal agent 52 对白色念珠菌表现出显着的抗真菌活性 Antifungal agent 52 影响白色念珠菌基底细胞膜通透性。

Tubulin inhibitor 38（化合物14）是一款强效的四唑基微管蛋白抑制剂，能够显著抑制细胞增殖。以100 nM浓度作用24小时后，该抑制剂能够引起有丝分裂停滞，特别是在G2 M期细胞周期阶段，进而诱导细胞凋亡。在HeLa、MCF7和U87 MG细胞系中，Tubulin inhibitor 38展现了较高的细胞毒性及选择性。

rac-Valsartan-d9 是 rac-Valsartan 的氘代化合物。rac-Valsartan 的 CAS 号为 137862-53-4。Valsarta 是一种血管紧张素 II 受体拮抗剂，有用于高血压和心力衰竭的研究潜力。