Catalog No.
Product Name
Application
Product Information
Product Citation
- Ranolazine is a partial fatty acid oxidation inhibitor, shifts ATP production from fatty acid to more oxygen-efficient carbohydrate oxidation.
- Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP).
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Factor Xa inhibitor
Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex.- Stefan Bittmann, .et al. , J Regen Biol Med, 2020, 2(2):1-3
- Daniël Verhoef, .et al. , Nat Commun, 2017, 8: 528 PMID: 28904343
- Mizuki Yamamoto, .et al. , Antimicrob Agents Chemother, 2016, Nov; 60(11): 6532-6539 PMID: 27550352
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PDE inhibitor
Roflumilast acts as a selective, long-acting inhibitor of the enzyme PDE-4.- Bo Liao, .et al. , Exp Ther Med, 2023, May 9;25(6):302 PMID: 37229319
- Zhongyuan Zhang, .et al. , Exp Ther Med, 2021, Dec;22(6):1398 PMID: 34650646
- Bing Zhong, .et al. , ACS Omega, 2021, Jan 26; 6(3): 2149-2155 PMID: 33521454
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PPAR agonist
Rosiglitazone works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin. -
PPAR agonist
Rosiglitazone maleate, an antidiabetic drug, works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.- Camilla Bean, .et al. , Nat Metab, 2021, Dec;3(12):1633-1647 PMID: 34873337
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HMG-CoA reductase inhibitor
Rosuvastatin (Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins. -
PDE4 inhibitor
(S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells. -
MAO Inhibitor
Safinamide Mesylate is mesylate salt of Safinamide, which selectively and reversibly inhibits MAO-B with IC50 of 0.45 μM. -
PDE5 inhibitor
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM. -
HMG-CoA reductase inhibitor
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM. - Sodium danshensu is a sodium salt of danshensu from the widely used Chinese herb Danshen (Salvia miltiorrhiza Bunge). In vitro and in vivo studies revealed that danshensu possessed diverse pharmacological effects, including relaxation of coronary artery, anticoagulation, protection of myocardial ischemia-reperfusion injury, and antiarrhythmia activities
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HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. - Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
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Phospholipase inhibitor
Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- Tanshinone IIA (TIIA) is one of the major extracts obtained from Salvia miltiorrhiza BUNGE, which has anti-inflammatory and anti-apoptotic effects on many diseases.
- Judith Schaf, .et al. , Cell Death Discov, 2023, May 19;9(1):172 PMID: 37202382
- Williams R, .et al. , Research Square, 2022, NOV 21
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Hydroxylase inhibitor
Tetrahydropapaverine, one of the TIQs and an analogue of salsolinol and tetrahydropapaveroline, has been reported to have neurotoxic effects on dopamine neurons. -
FTase inhibitor
Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor that inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive.- Xiaoming Liu, .et al. , J Immunother Cancer, 2022, Apr;10(4):e004399 PMID: 35483745
- Trilostane is an inhibitor of 3??-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
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PDE-5 Inhibitor
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction. -
CYP17 inhibitor
Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion. -
PDE Inhibitor
Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency Virus-1 Tat-Mediated activation of microglial cells. -
Hsp90 inhibitor
Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
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CYP17A1 inhibitor
TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme. -
FAAH inhibitor
URB597 is a relatively selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH).- Lakhan S Khara, .et al. , J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. , J Exp Biol, 2021, 21 JUNE
- Toshihiko Tsutsumi, .et al. , Biochim Biophys Acta Mol Cell Biol Lipids, 2020, Sep;1865(9):158761 PMID: 32629025
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CYP17 inhibitor
Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1). -
HSP90 Inhibitor
AT13387 is a targeted inhibitor of Hsp90,inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival.- Boucherat O, .et al. , Am J Respir Crit Care Med, 2018, Jul 1;198(1):90-103 PMID: 29394093
- Olivier Boucherat, .et al. , Sci Rep, 2017, 7: 4546 PMID: 28674407
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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Hsp90 inhibitor
PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.- Henry Aceros, .et al. , Life Sci, 2019, 2019 PMID: 30986447
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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CETP inhibitor
Anacetrapib (MK-0859) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. -
Retinoid X Receptor Ligand
Bexarotene is a highly selective retinoid X receptor (RXR) agonist. -
MAO B inhibitor
Rasagiline is a selective irreversible inhibitor of MAO-B (monoamine oxidase-B). -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
Hsp90 Inhibitor
PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).- Michael Heider, .et al. , Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
- Kale S, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2019, Sep 14 PMID: 31522240
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
FXR agonist
GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).- Dong-Hyun Kim, .et al. , Cell Death Dis, 2021, Apr; 12(4): 320 PMID: 33767132
- Takae K, .et al. , J Reprod Dev, 2018, Nov 16 PMID: 30449821
- TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
- Anirudh Sattiraju, .et al. , Immunity, 2023, Aug 8;56(8):1825-1843 PMID: 37451265
- Anirudh Sattiraju, .et al. , bioRxiv, 2022, March 04
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DBH inhibitor
Nepicastat hydrochloride is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
- Melina C Acosta, .et al. , Horm Behav, 2022, Jan;137:105086 PMID: 34808463