SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX), inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties[1]. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells[2].
AC-7954 is a selective nonpeptidic urotensin receptor agonist (EC50: 300 nM at the human UII receptor)[1].
Sandaracopimaric acid is a diterpenoid with anti-inflammatory effect. Sandaracopimaric acid reduces the contraction of phenylephrine-induced pulmonary arteries with an EC50 of 43.93 μM[1][2].
Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM. target: phosphodiesterase (PDE)[3]; IC 50: 0.036 microM; [3]In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) was 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increased global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [4]
Glycylglycylcysteine is a Thrombin Activatable Fibrinolysis Inhibitor (TAFI) inhibitor with a Ki of 0.99 μM and a IC50 of 9.4 μM in TAFI substrate assays. TAFI is a basic carboxypeptidase that functions as a fibrinolysis inhibitor through the cleavage of C-terminal lysine on partially degraded fibrin[1].
Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC50 of 0.28 μM[1].
2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation[1][2][3].
HNGF6A is a humanin analogue. HNGF6A increases glucose-stimulated insulin secretion and glucose metabolism, and has the potential for diabetes research. HNGF6A inhibits of ROS production during oxidative stress. HNGF6A can prevent endothelial dysfunction and atherosclerosis in vivo[1][2].
[Phe8Ψ(CH-NH)Arg9]-Bradykinin is a selective Bradykinin receptor B2 agonist (not cleaved by protein kinase I/II). [Phe8Ψ(CH-NH)Arg9]-Bradykinin has potential for the research of hypertension[1].
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo[1][2][3].
Cyclomorusin (Cyclomorusin A; Cyclomulberrochromene) is a prenylflavonoid with antiplatelet activity. Cyclomorusin also inhibits markedly collagen-induced platelet aggregation[1].
Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research[1].
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity[1]. Metyrosine is a very effective agent for blood pressure control[2].
Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2].
Lercanidipine hydrochloride is a calcium channel blocker of the dihydropyridine class.Target: Calcium ChannelLercanidipine is a calcium channel blocker of the dihydropyridine class, which works by relaxing and opening the blood vessels allowing the blood to circulate more freely around the body. Lercanidipine was effective and well-tolerated in patients with mild-to-moderate hypertension in the daily practice. The effectiveness and safety of the drug were independent of the degree of cardiovascular risk [1, 2].
NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker[1].
Fulvine is a pyrrolizidine alkaloid isolated from the seeds of Crotalaria fulva. Fulvine is hepatotoxic and can be used to induce hypertensive pulmonary vascular disease in vivo[1].
MRE-269-d6 is deuterium labeled MRE-269. MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
Ko-3290 is an antagonist of β-adrenoceptor, with cardioselectivity and antilipolytic effects in animals.
Benidipine is a potent and orally active calcium channel antagonist[1]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[2]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[3].
Bemfivastatin (PPD 10558) hemicalcium is an orally active lipid-lowering agent and HMG-CoA reductase inhibitor. Bemfivastatin hemicalcium enhances the activity of liver extracts. Bemfivastatin hemicalcium has no-observed adverse effect levels (NOAEL) with dosages of ≥320 mg/kg/d (rat developmental toxicity), ≥12.5 mg/kg/d (rabbit maternal toxicity), ≥25 mg/kg/d (rabbit developmental toxicity), respectively. Bemfivastatin hemicalcium can be used in the study of statin-related hypercholesterolemic myalgia in statin-intolerant patients.
(Rac)-Dobutamine-d6 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion[1][2][3][4].
4,6-Dioxoheptanoic acid-13C5 is the 13C labeled 4,6-Dioxoheptanoic acid[1]. 4,6-Dioxoheptanoic acid is a potent inhibitor of heme biosynthesis[2].
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM[1].
Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an endothelin receptor antagonist[1].
6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that inhibits CYP3A4 and is found in grapefruit juice and Seville orange juice[1].