Fructose is a simple ketonic monosaccharide found in many plants, where it is often bonded to glucose to form the disaccharide sucrose.
Rosuvastatin D3 (ZD 4522 D3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
ACTH (1-16) (human) (Adrenocorticotropic hormone (1-16)) is an ACTH fragment. ACTH (1-16) (human) improves cardiovascular function and survival in experimental hemorrhagic shock[1].
N-Acetylneuraminic acid-13C-1 is the 13C labeled N-Acetylneuraminic acid.
Flosequinan is a balanced vasodilator. Flosequinan not only significantly reduces systemic vascular resistance, but also significantly reduces the beating component of left ventricular afterload, characteristic impedance and arterial wave reflection, which can be used in the research of acute heart failure[1].
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.
CFM 1571 hydrochloride is the stimulator of the nitric oxide receptor, soluble guanylate cyclase (sGC) with an EC50 and IC50 of 5.49 μM and 2.84 μM, respectively. Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). CFM 1571 (hydrochloride) (compound 32) has the potential for the research of cardiovascular and other diseases[1][2].
Feretoside, a phenolic compound extracted from the barks of E. ulmoides, is a HSP inducer which act as cytoprotective agent.
PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC50 value of 7.57 μM.
CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM; has no effect on slow skeletal or cardiac myofibrils; significantly improves rotarod performance in exercise-intolerant LAD-HF rats. Spinal Muscular Atrophy (SMA) Phase 2 Clinical
TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM.IC50 value: 0.8 nM [1]Target: PDE10ATP-10 has extremely potent PDE10A inhibitory activity and highselectivity against other PDEs, and be active in the mouse behavioral model for positive symptoms. TP-10 demonstrats good in vitro and in vivo activity, the intrinsic clearance (CLint) of these compounds in mouse liver microsomes (MLM) was extremely high in assay (CLint>1000 mL/min/kg). [1]
(Rac)-Nebivolol-d8 ((rac)-R 065824-d8) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].
Spiraprilat is a potent angiotensin-converting enzyme (ACE) inhibitor. Spiraprilat has ability to improve left ventricular (LV) function and metabolism in anesthetized open-chest dogs with acute ventricular failure (ALVF)[1].
Ranolazine-d8 (CVT 303-d8) is the deuterium labeled Ranolazine. Ranolazine (CVT 303) 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)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Astragaloside A is one of the major active constituents of Astragalus membranaceus in Traditional Chinese Medicine; has been widely used to treat ischemic diseases.IC50 value: Target: in vitro: AS-IV treatment promotes umbilical vein endothelial cells (HUVEC) proliferation, migration, and tube formation. AS-IV treatment also activates JAK2/STAT3 and ERK1/2 signaling pathways, and up-regulates endothelial nitric oxide synthase (eNOS) expression and nitric oxide (NO) production [1]. Administration of astragaloside IV (16, 32, and 64 μM) 1 h prior to lipopolysaccharide stimulation dose-dependently attenuated cardiac hypertrophy induced by lipopolysaccharide. Further studies demonstrated that astragaloside IV inhibited the increment of the resting intracellular free Ca2+, and its effect was similar to verapamil [2]. ASI could inhibit cells apoptosis induced by high glucose (25mmol/L) in dose-dependent and time-dependent manners. ASI also inhibited high glucose-induced expression of TGF-β1 and activation of p38 MAPK pathway at the protein level. Furthermore, ASI increased HGF production in human tubular epithelial cells [3].in vivo: the growth of tumor was suppressed by AS-IV treatment in vivo. AS-IV also could down-regulate regulatory T cells (Tregs) and up-regulate cytotoxic T lymphocytes (CTLs) in vivo and in vitro[4]. As an in vivo model, mice subjected to unilateral ureteral obstruction (UUO) were administered AS-IV (20 mg/kg) by intraperitoneal injection for 7 days. AS-IV significantly alleviated renal mass loss and reduced the expression of α-smooth muscle actin, fibronectin, and collagen IV both in vitro and in vivo [5].
Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina[1][2][5].
Vitexin-2-O-rhamnoside, a main flavonoid glycoside of the leaves of Cratagus pinnatifida Bge, contributes to the protection against H2O2-mediated oxidative stress damage and has potential to treat cardiovascular system diseases[1].
Hexacosanoic acid-d4 is the deuterium labeled Hexacosanoic acid[1]. Hexacosanoic acid is a long-chain fatty acid related to various diseases such as adrenoleukodystrophy (ALD), adrenomyeloneuropathy (AMN) and atherosclerosis[2].
Olezarsen sodium is an N-acetyl-galactosamine-conjugated antisense oligonucleotide targeted to hepatic APOC3 mRNA to inhibit apolipoprotein C-III (apoC-III) production, in lowering triglyceride levels in patients at high risk for or with established cardiovascular disease.
DMAA is an indirect sympathomimetic amine. DMAA constricts blood vessels and raises blood pressure. DMAA can be used for neurological and cardiovascular disease research[1][2].
Benzoylpaeoniflorin is a natural product; may treat coronary heart disease by decreasing apoptosis.
AZD2906 is a selective glucocorticoid receptor (GR) agonist, with IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively. AZD2906 increases micronucleated immature erythrocytes (MIE) in the bone marrow of rats[1].
PCSK9-IN-17 is a PCSK9 inhibitor. PCSK9-IN-17 can be used for the research of cholesterol metabolism (WO2020150474A1, compound 105)[1].
SH-42 is a potent and selective inhibitor of human Δ24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice[1].
Felypressin is a Vasopressin 1 agonist, and will thus have effects at all Arginine vasopressin receptor 1As.target: Vasopressin 1 agonist;Felypressin is a synthetic hormone of the posterior pituitary lobe characterized by vasoconstrictor properties that is widely used in dental procedures.Felypressin has been widely added to local anesthetic solutions to increase the duration of the anesthetic effect and reduce the risk of toxicity during dental procedures.
α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer[1].
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism[1][2][3].
Setipafant is a platelet-activating factor (PAF) antagonist.
Zatebradine(UL-FS49) is a potent HCN channels antagonist, which decreased the heartbeat in a reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM.IC50 value: 10 uM(92% 92% inhibition of the hHCN1) [1]Target: hHCN channel antagonistThe pharmacological properties of hHCN1-mediated currents resembled those of native hyperpolarization-activated currents (I(h)), that is, blockade by Cs(+) (99% at 5 mm), ZD 7288 (98% at 100 microm) and zatebradine (92% at 10 microm) [1]. When voltage-clamp pulse trains were applied, cilobradine induced a use-dependent blockade of If that was stronger and faster than that with zatebradine. Recovery from blockade during prolonged hyperpolarization was significantly faster with zatebradine [2]. The selective HCN blocker zatebradine reduced the activity of oriens-lacunosum moleculare interneurons in wild-type but not HCN2(-/-) mice and decreased the frequency of spontaneous inhibitory currents in postsynaptic CA1 pyramidal cells [3].
DKI5, also known as (E)-N’-benzylidenehydrazinecarbothiohydrazide, is a LOX-1 inhibitor with an IC50 value of 22.5 μM[1].