RBx-7796 (sodium) is a competitive, highly selective, orally active 5-LO (IC50 = 3.5 mM for human 5-LO enzyme) inhibitor. RBx-7796 (sodium) can effectively inhibit 5-LO activity and LTB4 release. RBx-7796 (sodium) can significantly inhibit airway inflammation and bronchial constriction.

PF-3052334 is an orally active, hepatically selective HMG-CoA reductase inhibitor with an IC50 of 1.9 nM. PF-3052334 inhibits cholesterol synthesis, with IC50 values ​​of 0.9 and 730 nM in hepatocytes and muscle cells, respectively. PF-3052334 can be used to study hypercholesterolemia.

AT-1459 is a selective and orally active direct Thrombin inhibitor with a Ki value of 4.9 nM. AT-1459 exhibits excellent antithrombotic activity in both rat models of venous and arterial thrombosis. AT-1459 can be used for research on thrombosis-related diseases.

UK-356202 is a urokinase-type plasminogen activator (uPA) with a Ki value of 0.037 μM. UK-356202 can be used in research related to the topical treatment of chronic ulcerous wounds.

BMS-180431 is an inhibitor of HMG-CoA reductase (IC50: 43 nM).

Bay-y-1015 is an orally active quinoline-based 5-lipoxygenase inhibitor. Bay-y-1015 inhibits LTB4 and LTC4 synthesis. Bay-y-1015 can be used in the research of inflammatory diseases.

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.