Daprodustat
CAS 960539-70-2
Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor being developed for the treatment of anemia associated with chronic kidney disease.
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Bumetanide
CAS 28395-03-1
Bumetanide(Ro 10-6338; PF 1593) is an inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM.
PF-06282999
CAS 1435467-37-0
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.
Olodanrigan(EMA401)
CAS 1316755-16-4
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
PAMP-12(human, porcine)
CAS 196305-05-2
PAMP-12(human, porcine) is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.
Losmapimod
CAS 585543-15-3
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
Guanoclor
CAS 5001-32-1
Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
N6022
CAS 1208315-24-5
N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor with IC50 of 8 nM.
BMY 7378
CAS 21102-95-4
BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
Ralinepag
CAS 1187856-49-0
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
Cangrelor free acid
CAS 163706-06-7
Cangrelor is a P2Y12 inhibitor, and was approved in June 2015 as an antiplatelet drug for intravenous application. Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate.…
Droxidopa (L-DOPS,SM-5688)
CAS 23651-95-8
Droxidopa(L-DOPS, SM5688) is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); capable of crossing the protective blood–brain barrier.The acute administration of…
Ys-49
CAS 132836-42-1
YS 49 inhibits Ang II-stimulated proliferation of VSMCs via induction of HO-1.YS-49 is a novel positive inotropic isoquinoline compound. YS-49 has potential as a therapeutic strategy for the pathogenesis of Ang II-related vascular diseases such as…
EMD638683
CAS 1181770-72-8
EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 uM. The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drugs counteracting…
BMS813160
CAS 1286279-29-5
BMS-813160 is the first dual CCR2/CCR5 antagonist to enter clinical development for cardiovascular.
ML-277
CAS 1401242-74-7
ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the…
Cenupatide
CAS 1006388-38-0
Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor for treating disorders associated altered cell migration, such as cancer.
BAY 41-2272
CAS 256376-24-6
Activator of soluble guanylyl cyclase (sGC); acts at a nitric oxide (NO)-independent regulatory site in the sGC α1 subunit. Inhibits platelet aggregation (IC50 = 36 nM) and phenylephrine-induced contractions of rabbit aorta (IC50 = 0.30 μM). Also reduces…
Sparsentan(PS433540)
CAS 254740-64-2
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Levobetaxolol hydrochloride
CAS 116209-55-3
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
Heparin lithium salt
CAS 9045-22-1
Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII).
Sacubitril sodium
CAS 149690-05-1
Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the…
Avasimibe
CAS 166518-60-1
Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.
Cangrelor sodium
CAS 163706-36-3
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and…
Olinciguat (IW-1701)
CAS 1628732-62-6
Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay[1].
Balovaptan
CAS 1228088-30-9
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
MDI-2268
CAS 1609176-50-2
MDI-2268 (MDI2268) is a small-molecule, in vivo-active inhibitor of plasminogen activator inhibitor type-1 (PAI-1), demonstrates excellent pharmacokinetics, potent activity against vitronectin-bound PAI-1 in vivo, and efficacy in murine model of venous…
PD-123319 free base
CAS 130663-39-7
PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
SR59230A
CAS 174689-39-5
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
LY333531 Hydrochloride(Ruboxistaurin HCl)
CAS 169939-93-9
Ruboxistaurin hydrochloride is a selective and ATP-competitive PKCβ inhibitor, with IC50s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC50, 52 nM), PKCα (IC50, 360 nM), PKCγ (IC50, 300 nM), PKCδ (IC50, 250 nM), and has no…
Aprocitentan (ACT-132577)
CAS 1103522-45-7
ACT-132577 is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
NSC729477
CAS 229971-81-7
Exherin, also known as ADH-1, is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor…
SMS1-IN-1
CAS 1807943-38-9
SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis[1].
PF 6260933 dihydrochloride
CAS 1883548-86-4
PF 6260933 is a potent, selective and orally bioavailable MAP4K4 inhibitor with kinase IC50 of 3.7 nM, cell IC50 of 160 nM; possesses excellent kinome selectivity and suitable properties for in vivo pharmacological characterization; significantly improves…
Evacetrapib (LY2484595)
CAS 1186486-62-3
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
Isradipine
CAS 75695-93-1
Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and…
BQ-123
CAS 136553-81-6
BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) . 1) Reduces ischemia-induced ventricular arrhythmias in a rat model.2) BQ-123 prevents LPS-induced preterm birth in mice via the induction…
N-65828
CAS 501444-06-0
NCI-65828 (designated as N 65828) is a small-molecule inhibitor targeting angiogenin (ANG), a protein critical for angiogenesis and cellular proliferation. Its therapeutic potential stems from selective suppression of ANG's ribonucleolytic function, a…
Molidustat(BAY 85-3934)
CAS 1154028-82-6
Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
Retigabine dihydrochloride
CAS 150812-13-8
Retigabine (D-23129) is a novel antiepileptic compound with broad spectrum and potent anticonvulsant properties, both in vitro and in vivo. The compound was shown to activate a K+ current in neuronal cells. The pharmacology of the induced current displays…
Atorvastatin
CAS 134523-00-5
A competitive inhibitor of HMG-CoA reductase that acts as a lipid-lowering agent for prevention of events associated with cardiovascular disease.DyslipidemiaApproved
BMS-687453
CAS 1000998-59-3
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
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