GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50 of 2 nM and 40 nM for rTRPV4 and hTRPV4.
QCC374 is a selective agonist of IP[1].
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Acremoxanthone C is a potent calmodulin (CaM) inhibitor found in Purpureocillium lilacinum. Acremoxanthone C binds to the human calmodulin (hCaM) biosensor hCaM M124C-mBBr, with Kd of 18.25 nM[1].
FPL64176, a nondihydropyridine compound, is a potent agonist of L-type Ca2+ channels with an EC50 value of 16 nM[1][2].
(3-Carboxypropyl)trimethylammonium chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat.
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization[1].
GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
Ginsenoside Ro exhibits a Ca2+-antagonistic antiplatelet effect with an IC50 of 155 μM. Ginsenoside Ro reduces the production of TXA2 more than it reduces the activities of COX-1 and TXAS.
Small Cardioactive Peptide B (SCPB), a neurally active peptide, stimulates adenylate cyclase activity in particulate fractions of both heart and gill tissues with EC50s of 0.1 and 1.0 μM, respectively.
SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively[1].
UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of INa. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness[1][2][3].
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1)[1][1].
Vinpocetine(Cavinton; Ethyl apovincaminate) is a selective for PDE1 (IC50 = 21 μM). Also blocks voltage-gated Na+ channels.IC50 value:Target: PDE1; Na+ channel
Nattokinase is a potent fibrinolytic enzyme. Nattokinase can break down blood clots by directly hydrolyzing fibrin and plasmin substrate. Nattokinase can be used for the research of cardiovascular diseases[1].
Lercanidipine-13C,d3-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[1][2][3].
Prostaglandin D3 (PGD3) is a prostaglandin that acts as an inhibitor of platelet aggregation and a modulator of autonomic neurotransmission in humans[1].
Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs)[1]. Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately[2]. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects[3].
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function[1].
Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. It has also been investigated for use as an antiproliferative drug on drug-eluting stents.A 20-40 mg/h dose of FUT-175 prolonged coagulation time sufficiently in the instrumental blood of the extracorporeal circuit but not in the systemic blood. Its anticoagulant activity decreased immediately after hemodialysis. Therefore, we could manage all patients without any bleeding trouble during hemodialysis with FUT-175 as an anticoagulant. Although there were side effects of FUT-175, such as nausea, vomiting, itching and eruption, they were not serious, and FUT-175 could be administered without interruption. FUT-175 seems to be useful as an anticoagulant during hemodialysis for patients susceptible to bleeding.
EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. EMD 495235 shows anticoagulant activities[1].
Olmesartan-d4 Medoxomil (CS 866-d4) is the deuterium labeled Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
Tanshinol borneol ester, an angiogenesis stimulator, promoted multiple key steps of angiogenesis through Akt and MAPK signalling pathways. Tanshinol borneol ester has anti-ischemic and anti-atherosclerosis activities[1].
Dronedarone(Multaq) is a newer therapeutic agent with a structural resemblance to amiodarone and a better side effect profile; it is a multichannel blocker with antiadrenergic properties and has been evaluated in both rate and rhythm control strategies in the management of AF.IC50 value:Target: multichannel blocker
Trandolaprilate D5 is a deuterium labeled Trandolaprilate (Trandolaprilat). Trandolaprilate is an angiotensin-converting enzyme (ACE) inhibitor[1].
Sodium citrate dehydrate is an anticoagulant and also used as a buffer and food preservatives.
PD0176078 is a newly found N-type Calcium channel blocker.
MPO-IN-28 (Compound 28) is a myeloperoxidase (MPO) inhibitor with an IC50 of 44 nM.