10-Hydroxywarfarin, a metabolite of (R)-(+)-Warfarin, is a CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR) inhibitor with IC50s of 1.6 µM and 80 ng/mL, respectively.

ZGL-18 is an uncoupling protein 1 (UCP1)-inspired mitochondrial uncoupler. ZGL-18 activates brown adipocytes and reduces mitochondrial membrane potential.

SHO1122147 (Compound 7m) affects the mitochondrial electron transport chain, exhibits mitochondrial uncoupling activity (EC50=3.6 μM), and increases the oxygen consumption rate (OCR=69%) and promotes cellular respiration. SHO1122147 is orally active, and can be used in reaearch of obesity and metabolic dysfunction-associated steatohepatitis (MASH).

S-15176 is an inhibitor of the mitochondrial permeability transition pore (PTP). S-15176 inhibits mitochondrial swelling induced by tert-butylhydroperoxide with an IC50 value of 45.7 μM. S-15176 inhibits PTP opening, prevents mitochondrial membrane potential dissipation and NAD(P)H oxidation, and increases mitochondrial calcium loading capacity. S-15176 is promising for research of ischemia-reperfusion injury.

PENAO is a potent tumour cell mitochondrial toxin. PENAO inactivates tumor cell mitochondria by targeting inner-membrane adenine nucleotide transferase.

LH1513 is a dioxalate derivative of l-lysine that inhibits CaOx crystallization with better activity than citrate and pyruvate. LH1513 has potential preventive activity in hyperoxaluria models and effectively prevents urinary CaOx crystal formation in Agxt knockout mice. AGXT-1 is a mitochondrial protein involved in metabolism.

BE2647 is a selective inhibitor for mitochondrial pyruvate carrier (MPC) with an EC50 of 70 nM. BE2647 exhibits good metabolic stability in mouse liver microsomes. BE2647 can be used in research of metabolic diseases, non-alcoholic fatty liver disease (MASLD), or non-alcoholic steatohepatitis (MASH).

Bac-429 (compound 23) is a N-acyl amino acid analog that stimulates mitochondrial respiration.

AK-4 is a glucose-lowering agent, acting function as a mitochondrial uncoupler.

Heparin is a highly sulfated polysaccharide primarily used as an anticoagulant, which works mainly by inhibiting thrombin (FIIa) and/or factor Xa (FXa). It is commonly used to prevent and treat thromboembolic conditions such as deep vein thrombosis and pulmonary embolism. It also plays roles in inflammation, angiogenesis, and growth factor signaling, with potential therapeutic applications in cancer treatment and allergic conditions.

YD-3 is a platelet activation inhibitor. YD-3 inhibits Thrombine-induced rabbit platelets aggregation (IC50: 28.3 μM) and phosphoinositol production. In addition, YD-3 also inhibits Trypsin-induced platelet aggregation in human and rabbit with the IC50 of 38.1 μM and 5.7 μM, respectively, but does not affect the proteolytic activity of trypsin.

(2R)-Atecegatran ((2R)-AZD-0837; (Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab)) is a thrombin inhibitor. (2R)-Atecegatran can be used in research related to thromboembolic disorders.

Ro 23-9358 is a potent secretory phospholipase A2 inhibitor with anti-inflammatory activity.

LY433771 (LSN433771) (Compound 8) is a type X secretory phospholipase A2 (sPLA2) inhibitor with an IC50 value of 3 nM, which can be used in the study of cardiovascular diseases.

GK420 (AVX420) is a potent inhibitor of cytosolic phospholipase A2α (cPLA2α), with the XI(50) of 0.0016. GK420 inhibits arachidonic acid release with the EC50 of 0.09 μM. GK420 plays an important role in cancer research.

DPTIP hydrochloride is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC50 of 30 nM.

C10 Bisphosphonate is an inhibitor for acid sphingomyelinase. C10 Bisphosphonate is promising for research of inflammatory lung diseases, cystic fibrosis and atherosclerosis.

BRI-50460 is an inhibitor of cytosolic calcium-dependent phospholipase A2 (cPLA2) that has the ability to penetrate the blood-brain barrier, with an IC50 of 0.88 nM. BRI-50460 exerts the activities of regulating neuroinflammation and restoring lipid homeostasis by inhibiting cPLA2, regulating the downstream inflammatory lipid signaling pathway, and alleviating the effects of amyloid β42 oligomers on the activation of cPLA2, the hyperphosphorylation of tau protein, and the reduction of synapses and dendrites. BRI-50460 can be applied to the research in the fields of Alzheimer's disease and other neurodegenerative diseases.

ABC47 is a potent inhibitor of serine hydrolases. ABC47 shows IC50s of 0.03 and 0.1 μM for ABHD4 and ABHD3, respectively. ABC47 plays an important role in infantile neuronal ceroid lipofuscinosis research.

Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, with an IC50 of 3.95 ng/mL. Xanthoanthrafil can be used for the research of erectile dysfunction.

Pyrazole N-Desmethyl sildenafil (Compound 10) is an analog of Sildenafil.

PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.

P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F.

MP 518 is a PDE inhibitor with antihypertensive properties. MP 518 can inhibit cAMP degradation, causing an increase in ICa, and can also antagonize β-adrenergic stimulation, exerting vasodilation.

Desmethyl thiosildenafil is a phosphodiesterase type 5 (PDE5) inhibitor[1].

Desethyl Sildenafil (Sildenafil impurity C) is the impurity of Sildenafil (IC50 of 134.29 μM).

Cipamfylline is a PDE4 inhibitor that can cause PDE4A4 to accumulate in specific areas of the cell through interaction with the ubiquitin scaffolding protein p62. Cipamfylline can be used in the research of atopic dermatitis.

BMS-341400 mesylate (Compound 6) is an orally active and a selective phosphodiesterase 5 (PDE5) inhibitor, with IC50 of 0.3 nM. BMS-341400 mesylate can be used for research of erectile dysfunction.

BC8-15 is a PDE inhibitor with IC50 values of 0.28, 0.22, and 6.46 µM for inhibiting PDE8A, PDE4A, and PDE7A, respectively. BC8-15 can enhance steroidogenesis in mouse Leydig cells.

ASP9831 is an orally active PDE4 inhibitor. ASP9831 inhibits LSP-induced TNF-α production and has anti-inflammatory activity. ASP9831 can be used in fatty liver disease research.