Ramiprilat diketopiperazine (Ramipril diketopiperazine acid; Impurity K) is an impurity of Ramiprilat. Ramiprilat, an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor.

Ramipril diketopiperazine is an impurity in the ACE inhibitor Ramipril.

Quinapril is a potent, orally active, non-peptide and nonsulfhydryl inhibitor of angiotensin-converting enzyme (ACE). Quinapril specifically interrupts the conversion of angiotensin I to angiotensin II in both plasma and tissue. Quinapril is enzymatically hydrolyzed to a pharmacologically active diacid form quinaprilat. Quinapril is efficacious in hypertensive models.

Perindopril L-arginine is an orally active and selective angiotensin-converting enzyme (ACE) inhibitor. Perindopril L-arginine reduces the production of angiotensin II by inhibiting ACE, thereby dilating blood vessels, lowering blood pressure, and also exerting activities such as vasculoprotection and antithrombosis. Perindopril L-arginine is promising for research of cardiovascular diseases.

AD015 is a angiotensin-converting enzyme (ACE) and neprilysin (NEP) dual inhibitor. AD015 inhibits NEP, nACE and cACE with IC50s of 0.009, 0.019 and 0.0008 μM, respectively.

SDUY816 is an oral active dual APN/NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. SDUY816 exhibits analgesic effects and demonstrates good safety and pharmacokinetic profiles, with an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral administration, 10 mg/kg). SDUY816 has potential applications in the research of neuropathic pain disorders.

LYS006 hydrochloride is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) extracted from patent WO2015092740A1, example 29, has an IC50 of 2 nM. LYS006 hydrochloride can be used for the research of inflammatory and autoimmune disorders.

DG013B formate is an epimer of DG013A.

DG013B is an epimer of DG013A.

DG013A (formate) is a phosphinic acid tripeptide mimetic inhibitor. DG013A (formate) displays significantly weak affinity for both ERAP1 (IC50=33 nM) and ERAP2 (IC50=11 nM). DG013A (formate) can be used for the research of autoimmune disease and cancer.

BDM_92499 is a nanomolar selective IRAP inhibitor, with an IC50 of 3.4 nM. BDM_92499 also inhibits ERAP1 and ERAP2, with IC50 values of 0.46 μM and 4.2 μM, respectively.

Arphamenine A is an aminopeptidase B inhibitor found in Chromobacteriuin violaceum HMG361-CF4. Arphamenine A can inhibit the activity of aminopeptidase B, and can inhibit sarcoma 180 and invasive micropapillary carcinoma (IMC) cancer.

Apstatin TFA is a potent aminopeptidase P (APP) inhibitor with Ki values of 2.6, 0.64 µM for rat and human APP, respectively. Apstatin TFA shows cardioprotection.

WF-3681 (compound 1) is an aldose reductase inhibitor and a fungal metabolite.

RJG-2051 is a selective covalent aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC50 value of 13 nM. RJG-2051 interferes with the metabolic process of substrates such as androgens, estrogens, and prostaglandins by AKR1C3. RJG-2051 is promising for research of cancers.

M79175 is an aldose reductase inhibitor that can be used in the study of early diabetic retinopathy.

(Rac)-Fidarestat ((Rac)-SNK 860) is the racemate of Fidarestat-resistant hepatitis B.

Mirivadelgat is an activator of aldehyde dehydrogenase 2 activator. Mirivadelgat is promising for research of interstitial lung disease-pulmonary hypertension and cancers.

DG 381B (compound 62) is a 11β-HSD1 and 11β-HSD2inhibitor.

NAMPT activator (NAT-5r) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 180 nM, 3-fold improved activity over NAT.NAMPT activator (NAT-5r) had no effect on NMNAT1 enzyme activity, both NAMPT mutants of K189R and K189A reduced the binding affinity of NAT-5r.NAMPT activator (NAT-5r) treatment significantly enhanced NAD content in NAMPT-WT cells, but not in NAMPT-CRISPR cells.Treatment of NAT-5r at 3 μM concentrations for 4 h induced significant elevation of cellular NAD.NAMPT activator (NAT-5r) induced subsequent metabolic and transcriptional reprogramming, promoted proliferation and maintain the self-renewal of NSCs and protects peripheral sensory neurons from paclitaxel-(PTX) induced damage in mouse model.

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.

BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM. BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3. BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a dose dependent manner. BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.

Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC).

NSC45586 sodium is a selective inhibitor targeting the PP2C phosphatase domain within both PHLPP1 and PHLPP2 proteins. By blocking these phosphatases, it enhances AKT activation in neuronal cells.

ALLM (Calpain Inhibitor) is cell-permeable, peptide aldehyde inhibitor of calpains and cathepsins.

Dabigatran etexilate mesylate (BIBR 1048MS) serves as the ​orally bioavailable prodrug of the active anticoagulant dabigatran. Following absorption, this precursor compound undergoes ​enzymatic conversion to release dabigatran - a highly ​selective, reversible direct thrombin inhibitor (DTI) with exceptional potency (Ki = ​4.5 nM).

BIBR-1048 (Dabigatran) represents a breakthrough in anticoagulant therapy as a ​potent, selective direct thrombin inhibitor.

ADAM17 inhibitor SN-4 is a newly identified, highly specific inhibitor of ADAM17 (A disintegrin and metalloproteinase 17), demonstrating potent activity in blocking TNF-α cleavage in cellular assays with an IC50 value of 3.22 µM. This compound exhibits slightly greater efficacy compared to marimastat, a well-established ADAM17 inhibitor. In vitro studies reveal that SN-4 effectively suppresses ADAM17-mediated cleavage of tumor necrosis factor α (TNF-α) and CD44, while showing no significant impact on ADAM10 activity. Additionally, SN-4 has been shown to inhibit cellular invasion, highlighting its potential as a targeted therapeutic agent for modulating ADAM17-related pathways.

N4-Acetylcytidine triphosphate is efficiently used as a substrate in T7 Polymerase-catalyzed in vitro transcription and can be incorporated into multiple templates.

NCATS-SM7270 is a highly specific small molecule inhibitor of NADPH oxidase 2 (NOX2), exhibiting an IC50 value of 2.1 µM in polymorphonuclear leukocytes (PMN). It effectively inhibits NOX2 activity in both primary human and mouse granulocytes, demonstrating its targeted and potent mechanism of action.