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Metabolic Enzyme/Protease

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Cat. No. Product Name Field of Application Chemical Structure
DC76852 SID 24785302
SID 24785302 is an inhibitor for hexokinase. SID 24785302 inhibits glycolysis, regulates mitochondrial functions, thereby inhibiting the replication of mutant mtDNA.
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DC76851 SE 175
SE 175 is an organic nitrate compound that acts as an NO donor in vivo following reductive transformation of the nitrate group to nitric oxide. SE 175 stimulates endothelial soluble guanylate cyclase and induces aortic vasorelaxation with an EC50 of 0.20 µM.
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DC76850 AZ513
AZ513 is a reversible FAAH inhibitor with an IC50s of 551 nM and 27 nM for human FAAH and rat FAAH, respectively. AZ513 inhibits Anandamide.
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DC76849 MeO-Suc-Ala-Ala-Pro-Ala-CMK
MeO-Suc-Ala-Ala-Pro-Ala-CMK (MSACK) is an inhibitor of human neutrophil elastase (HNE), with an IC50 of 20.3 μM. MeO-Suc-Ala-Ala-Pro-Ala-CMK can inhibit the hydrolysis of substrates such as elastin in lung tissue by HNE. MeO-Suc-Ala-Ala-Pro-Ala-CMK can be used in the research of related diseases such as chronic obstructive pulmonary disease (COPD).
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DC76848 Methylspinazarin
Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT, IC50 = 0.8 μg/ml) that can be isolated from Streptomyces. Methylspinazarin is selective for COMT over tyrosine hydroxylase.
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DC76847 Verducatib
Verducatib is a cathepsin inhibitor.
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DC76846 TB-9
TB-9, a Tasiamide B derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.
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DC76845 FGA139
FGA139 is a cysteine proteases inhibitor with IC50 values of 4.98/3.14 μM for cathepsin B/L. FGA139 reduces LPS-induced NO production in RAW264.7 cells and tumor necrosis factor (TNFα) levels in microglia, and has anti-oxidative stress and anti-inflammatory activities. FGA139 promotes the secretion of neuroprotective metabolites purine and linoleic acid by LPS-stimulated microglia. FGA139 can be used in neuroinflammatory diseases research.
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DC76844 Abz-FRF(4NO2)
Abz-FRF(4NO2) is an Abz-tripeptide substrate commonly used for studying the activity of enzymes, especially cysteine proteases such as Cathepsin X.
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DC76843 Acetazolamide sodium
Acetazolamide sodium is an inhibitor of carbonic anhydrase (CA) IX with an IC50 of 30 nM for hCA IX and also inhibits hCA II with an IC50 of 13 nM. It possesses diuretic, antihypertensive, and anti-gonococcal properties.
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DC76842 SH7s
SH7s is a potent carbonic anhydrases inhibitor, with Kis of 15.9 and 55.2 nM for hCA IX and hCA XII, respectively. SH7s is also a hypoxia-mediated chemo-sensitizing agent in colorectal cancer cells.
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DC76841 DOTA-XYIMSR-01
DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide, is a Vps34 inhibitor.
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DC76840 Chlorzolamide
Chlorzolamide (CL 13580) is a carbonic anhydrase (CA) inhibitor. Chlorzolamide has an effect on the skeletal muscle of rats, which can reduce the tetanic contraction force of soleus and extensor digitorum longus and prolong the relaxation time and peak time of muscle contraction. In addition, Chlorzolamide inhibits tumor cell proliferation and has antitumor activity.
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DC76839 (Rac)-Sezolamide
(Rac)-Sezolamide (MK-927 (free base); (Rac)-MK 417 (free base)) is a carbonic anhydrase inhibitor (CAI) (Ki: 12.0 nM). (Rac)-Sezolamide has a topical intraocular pressure (IOP) lowering effect. (Rac)-Sezolamide can be used in glaucoma research.
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DC76838 Rev 6207 free base
Rev 6207 (free base) is a potent non-thiol angiotensin I converting enzyme inhibitor. Rev 6207 (free base) has comparable antihypertensive activity to Enalapril in awake monkeys with high renin activity and can be used in the study of hypertensive diseases.
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DC76837 Ramiprilat diketopiperazine
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.
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DC76836 Ramipril diketopiperazine
Ramipril diketopiperazine is an impurity in the ACE inhibitor Ramipril.
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DC76835 Quinapril
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.
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DC76834 Perindopril L-arginine
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.
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DC76833 AD015
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.
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DC76832 SDUY816
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.
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DC76831 LYS006 hydrochloride
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.
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DC76830 DG013B formate
DG013B formate is an epimer of DG013A.
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DC76829 DG013B
DG013B is an epimer of DG013A.
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DC76828 DG013A formate
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.
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DC76827 BDM_92499
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.
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DC76826 Arphamenine A
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.
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DC76825 Apstatin TFA
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.
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DC76824 WF-3681
WF-3681 (compound 1) is an aldose reductase inhibitor and a fungal metabolite.
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DC76823 RJG-2051
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.
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