Others

Azelnidipine, (S)-, is an L-type calcium channel blocker (CCB). Studies have shown that in patients with hypertension (HT) and heart failure preserved ejection fraction (HFpEF), azelnidipine improved the severity of HF and cardiac sympathetic nerve activity compared with cilnidipine, an N-type CCB (Cat#326734).

Momelotinib HCl is a JAK1/2 inhibitor, reducing anemia in myelofibrosis (MF) patients.

AZD-4121 tert-butylammonium is an oral cholesterol absorption inhibitor targeting NPC1L1 for the treatment of dyslipidaemia.

BP-1-108 is a potent and selective STAT5 inhibitor.

MF-095 is a control probe for MF-094, which is a potent inhibitor of ubiquitin specific protease 30.

Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.

RPR203494 is a pyrimidine analogue of the p38 inhibitor RPR200765A with an improved in vitro potency.

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, in an aggressive syngeneic model, demonstrated superior tumor growth inhibition and a positive therapeutic index relative to combretastatin A-4 phosphate (CA4P).

Bupivacaine is a BK/SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

CD4 (81-92) is a peptide that was previously found to inhibit gp120 binding, HIV-1 infectivity, and syncytium formation.

tabilautide 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T68148，CAS号为 78088-46-7。

Imidazole mustard is an inhibitor of purine nucleoside synthesis.

SCHEMBL12616233 is a novel inhibitor of SARS-CoV-2 main protease (MPro).

Cefmenoxime sodium is the ssalt form of Cefmenoxime (free base), a cephalosporin antibiotic administered intravenously or intramuscularly. It is active against most common gram-positive and gram-negative microorganisms. It is a potent inhibitor of Enterobacteriaceae, and is resistant to beta-lactamase-initiated hydrolysis. The drug has a high success rate against many types of infection.

Dmp 811 is an angiotensin II receptor antagonist.

AY 25674 is a drug with antiallergic properties which has been shown to inhibit passive anaphylaxis in rat.

Nutlin-1 is a p53-MDM2 binding inhibitor, p-Glycoprotein (p-gp) transport substrate, and antitumor agent.

Chlorodenafil is a related compound of Sildenafil -- a phosphodiesterase inhibitor.

U 66985 is a Platelet-activating factor (PAF) receptor antagonist that inhibit the electrophysiological effects of PAF.

UH 232 is a dopamine receptor antagonist.

MRLB-223 is a potent inhibitor of HDAC1 and HDAC2.

AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished macrophage infiltration into BAL fluid induced by tobacco smoke inhalation in the mouse.

Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

TH251 is a highly selective antagonist of LIMK1 and LIMK2 (LIMK1/2).

Protease-Activated Receptor-1 antagonist 2 是一种选择性蛋白酶激活受体-1 (PAR-1) 拮抗剂，口服活性，IC50值为7 nM。该化合物具有优良的药代动力学特性，适用于心血管疾病 (CVD) 如动脉粥样硬化和再狭窄的研究。

Idaverine is an M2-selective muscarinic antagonist.

Methyl gerfelin通过与三种关键细胞蛋白乙二醛酶 1 (GLO1)、固醇结合蛋白 2 (SCP2) 和富含谷氨酰胺的四肽重复蛋白 A (SGTA) 结合，抑制破骨细胞的分化。研究表明，Methyl gerfelin是一种与类黄酮相关的强效GLO1抑制剂。

Downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.

IRE1α kinase-IN-4 (compound 6) 是一种有效的IRE1α抑制剂，Ki 为 140 nM。IRE1α kinase-IN-4 是 IRE1α 的 ATP 竞争性配体。

DK-139 is an inhibitor of NF-kappaB-mediated GROalpha expression, suppressing the TNFalpha-induced invasive capability of MDA-MB-231 human breast cancer cells.

Lupitidine hydrochloride inhibits nocturnal acid secretion.

EMD-23448 is a dopamine autoreceptor agonist as potential antipsychotics.

Novembichin is a nitrogen mustard agent that crosslinks with DNA, causing inhibition of DNA synthesis.

V11294A is a novel PDE4 inhibitor. A single oral 300 mg dose of V11294A administered to healthy volunteers results in plasma concentrations adequate to inhibit activation of inflammatory cells ex vivo, which persists for at least 24 h without any adverse reactions

8-bromo NAD+ 作为循环ADP-核糖（cADPR）抑制剂8-bromo cADPR的前药形式，通过CD38转化为8-bromo-cADPR。在1 mM浓度下，8-bromo NAD+ 阻止由N-formyl-Met-Leu-Phe (fMLP) 在分离的小鼠骨髓衍生的中性粒细胞内引起的细胞内钙水平增加和趋化作用。同时，在100 µM浓度下使用，减少了小鼠原代小胶质细胞中LPS诱导的亚硝酸盐产生以及TNF-α和IL-2的分泌。

Kahweol linoleate is a semi-syntetic derivative of kahweol, a natural product found in coffee beans. It exhibits a wide variety of biological activities, including inhibiting RANKL-induced osteoclast generation, inducing cell cycle arrest and apoptosis in oral squamous cell carcinoma cells, preventing aflatoxin B1 induced DNA adduct formation, and suppressing H2O2-induced DNA damage and oxidative stress.