OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC50 values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC50s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.

A-350619 is a novel sGC activator. A-350619 increases intracellular cGMP levels. A-350619 significantly induces penile erection.

(R)-Xanthoanthrafil is a phosphodiesterase-5 (PDE5) inhibitor. (R)-Xanthoanthrafil selectively inhibits PDE5, increasing cyclic guanosine monophosphate (cGMP) levels, leading to smooth muscle relaxation and promoting penile erection. (R)-Xanthoanthrafil can be used to study erectile dysfunction.

CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor.

FR-182980 is an orally active ACAT1 inhibitor (IC50: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis.

CL-283796 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.

(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.

(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

Ciprokiren (Ro 44-9375) is a Renin inhibitor with IC50s of 0.07 and 0.65 nM for hRenin in buffer and plasma, respectively. Ciprokiren be applied transdermally with similar hemodynamic effects without decrease of plasma renin activity or plasma immunoreactive angiotensin II. Ciprokiren has antihypertensive efficacy and can be used for hypertension research.

NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.

ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.

ACP3 ligand 1 (compound I11a) is a ligand against Acid Phosphatase 3 (ACP3, ACPP). ACP3 ligand 1 interacts with ACP3 expressed on the surface of tumor cells for in vivo pharmaco-delivery applications.

Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC50 = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.

BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC50 = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC50 = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease.

RPR 130737 is a selective, potent and competitive inhibitor for factor Xa with a Ki of 2.4 nM. RPR 130737 shows selectivity of more than 1000-fold over thrombin, activated protein C, plasmin, tissue-plasminogen activator and trypsin. RPR 130737 can prolong plasma activated partial thromboplastin time and prothrombin time. RPR 130737 shows no effect on platelet aggregation. RPR 130737 can be used for the research of cardiovascular disease, such as thrombosis.

KD-027 (SLx-2101) is a Phosphodiesterase 5 (PDE5) inhibitor. KD-027 can be used for endothelial dysfunction, and hypertension research.

AD-5467 is a potent and selective aldose reductase inhibitor. AD-5467 exhibits antidiabetic effect. AD-5467 can be used for the research of metabolic disease, such as diabetes.

Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.

SC-57461 is a potent, selective, and orally effective LTA4 hydrolase (Ki = 23 nM and 27 nM) inhibitor. SC-57461 can significantly inhibit edema. SC-57461 is commonly used in the study of inflammatory skin conditions.

BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.

LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.

MOL-6131 is a highly selective, reversible tryptase inhibitor, with a Ki of 45 nM. MOL-6131 significantly reduces the following features of allergic airway inflammation: eosinophil infiltration in lung tissue, goblet cell hyperplasia and mucus occlusion of airways.

CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases.

HOE-288 is an orally active angiotensin-converting enzyme (ACE) inhibitor. HOE-288 can be used for the research of neurological disease.

BLX-2477 is a potent and selective 15-lipoxygenase-1 (15-LOX-1) inhibitor with an IC50 value of 99 nM. BLX-2477 can inhibit the generation of inflammatory lipid mediators such as 15-hydroxy-eicosatetraenoic acid (15-HETE). BLX-2477 can be used for the research of inflammation and immunology.

Populin (Populoside) is a phenolic glucoside with antioxidant activities. Populin inhibits aldose reductase with an IC50 of 18.55 μM. Populin shows IC50s of 6.76 µM and 1.69 mM in DPPH radical-scavenging and ABTS ·+ radical-scavenging assays. Populin also inhibits D-Sorbitol accumulation.Populin has the potential to be used in the study of diabetic complications.

FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the research of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.

DPC423 free base is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits Kis of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base has demonstrated antithrombotic effects in animal models, and when used in combination with Aspirin, it shows a strong synergistic effect. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis.

MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.

sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF).