diseases

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Oxolamine citrate (AF-438 citrate) is a cough suppressant that is able to be used as a generic drug in many jurisdictions.

Tylosin tartrate, a macrolide antibiotic, is approved for the control of mycoplasmosis in poultry.

Sulfachloropyrazine sodium(Sulfachloropyrazine) is an antiprotozoal,with antibacterial and anticoccidial effects

SM-324405 is an agonist of TLR7.

Tylosin (Tylosine) is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Magnesium Lithospermate B is a natural product activates eNOS and ameliorates endothelial dysfunction in diabetes by enhancing vasodilation in addition to reducing oxidative stress, it can protecte cardiomyocytes from ischemic injury through specific inhibition of TAB1-p38 apoptosis signaling.improves renal failure.

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.

β-N-Methylamino-L-alanine hydrochloride (L-BMAA hydrochloride) is a neurotoxin produced by cyanobacteria that may contribute to the development of amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.

(-)-Huperzine A (HupA) , an active Lycopodium alkaloid extracted from the traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

Delapril hydrochloride (indalapril) is a prodrug; it is converted into two active metabolites, 5-hydroxy delapril diacid and delapril diacid. These metabolites bind completely to and inhibit angiotensin-converting enzyme (ACE), hence blocking angiotensin I to angiotensin II conversion.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.

OsMundacetone (4-(3,4-Dihydroxyphenyl)-3-buten-2-one) is a natual product isolated from Rhizoma osmundae.

yGsy2p-IN-1 is a potent inhibitor of yeast glycogen synthase 2 (yGsy2p) and human glycogen synthase 1 (hGYS1). Additionally, yGsy2p-IN-H23, a pyrazole inhibitor, is utilized in the treatment of glycogen storage diseases (GSDs).

CID44216842 (KUC103479N-02) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.

Azelaprag (Example 263.0) is a candidate active molecule (EC50= 0.32 nM) for an apelin receptor agonist. Azelaprag can be used to treat nervous system diseases, cardiovascular diseases.

DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.