Deferiprone-d3 is the deuterium labeled Deferiprone. Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload[1][2].
Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery[1][2].
GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects[1].
Tranexamic acid (Transamin) is an antifibrinolytic for blocking lysine-binding sites of plasmin and elastase-derived plasminogen fragments with IC50 of 5 mM. Target: OthersTranexamic acid is a synthetic derivative of the amino acid lysine. Tranexamic acid is frequently used in surgeries with high risk of blood loss such as cardiac, liver, vascular and large orthopedic procedures. Its oral form is now being evaluated for use in outpatient conditions involving heavy bleeding.Toxicity/Adverse event: Rare in general, including gastrointestinal effects, dizziness, fatigue, headache, and hypersensitivity reactions. Use of tranexamic acid has a potential risk of thrombosis.
Praeruptorin C is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2′ value of 5.7[1].
Yohimbic acid hydrate is an amphoteric demethylated derivative of Yohimbine (HY-12715). Yohimbic acid hydrate exhibits vasodilatory action. Yohimbic acid hydrate also can be used for the research of osteoarthritis (OA)[1][2][3].
Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
N-TRANS-CaffeoyLtyramine is an effective inflammatory response regulator, which has antioxidant activity and anticoagulation effects[1].
Rivipansel (GMI-1070) is a potent E-selectin antagonist. Rivipansel prevents interaction between leukocytes and vascular endothelium. Rivipansel has the potential for the research of sickle cell vaso-occlusive crisis[1][2].
Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist.Target: α1-adrenoceptor; 5-HT1A receptorUrapidil hydrochloride is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system [1]. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system. Several studies have suggested that oral urapidil is effective and well tolerated when used as second-line therapy in patients with BP inadequately controlled with other agents. Urapidil has also been shown to improve glucose and lipid metabolism in hypertensive patients with concomitant diabetes and/or hyperlipidemia [2].
Citric acid triammonium (Triammonium citrate) is formed by Citric acid (HY-N1428) reacting with ammonia in a molar ratio of 1:3. Citric acid triammonium can be used as the carbon source to prepare carbon quantum dots (CDs). Citric acid triammonium with higher nitrogen components might promote the nitrogen-based functional groups in CDs, leading to a more efficient emission-color tunability[1][2].
Tonlamarsen sodium is a angiotensinogen synthesis reducer, with antihypertensive activity[1].
2,3,4,6,8-Pentahydroxy-1-methylxanthone is a xanthone derivative of Wardomyces anomalus. 2,3,4,6,8-Pentahydroxy-1-methylxanthone shows significant antioxidant activities. 2,3,4,6,8-Pentahydroxy-1-methylxanthone is inhibitors of p56lck tyrosine kinase. 2,3,4,6,8-Pentahydroxy-1-methylxanthone can be used to treat cardiovascular disease[1].
MG-262 is a reversible proteasome inhibitor with diverse biological activities[1][2][3].
RXFP1 receptor agonist-3 (Example 223) is a RXFP1 receptor agonist. RXFP1 receptor agonist-3 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 2 nM[1].
Quinidine is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine can be used for malaria research[1][2][3].
Vitamin K is a group of fat soluble vitamins, important for the function of numerous proteins within the body, such as the coagulation factors, osteocalcin and matrix-Gla protein.
(+)-Osbeckic acid is a vasorelaxatant that can be isolated from Tartary Buckwheat. (+)-Osbeckic acid has a potent vasorelaxant effect in Sprague-Dawley rat thoracic aorta rings with an EC50 of 887 μM[1].
Budiodarone (ATI-2042) is an analogue of Amiodarone (HY-14187) with a half-life of 7 h. Budiodarone inhibits sodium, potassium, and calcium ion channels. Budiodarone is an antiarrhythmic agent and can be used for the research of atrial fibrillation[1].
SU5408 is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
QH536 (Compound 29) is a potent HMGCR degrader with an EC50 of 0.22 μM. QH536 has no side-effect of inducing cholesterol accumulation in cells. QH536 shows anti-inflammatory and can be used for cardiovascular disease and nonalcoholic steatohepatitis research[1].
ACTH (6-24) (human) (Adrenocorticotropic hormone (6-24)) is an ACTH fragment. ACTH (6-24) (human) is a competitive inhibitor of steroidogenesis induced by ACTH (1-39) and ACTH (5-24) (Kd:13.4 and 3.4 nM). ACTH (6-24) (human) inhibits corticosterone production and cAMP accumulation induced by hPTH 1-34[1][2].
L-Aspartic acid-1,4-13C2,15N is the 13C- and 15N-labeled L-Aspartic acid. L-Aspartic acid is is an amino acid, shown to be a suitable prodrug for colon-specific drug deliverly.
Alytesin, a bombesin-like peptide, is found in extracts of the skin of Alytes obstetricans. Alytesin reduces gastric acid secretion and induces hypertension. Alytesin also induces short-term anorexigenic effects in neonatal chicks[1][2][3]
LY285434 is a suitable angiotensin II receptor antagonist.
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis[1][2][3].
RXFP1 receptor agonist-7 (Example 2) is a RXFP1 receptor agonist. RXFP1 receptor agonist-7 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 4.2 nM[1].
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine (Mepirodipine) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
5-Aminolevulinic acid-13C (5-ALA-13C) is the 13C-labeled 5-Aminolevulinic acid. 5-Aminolevulinic acid (5-ALA) is a non-protein amino acid that plays a rate-limiting role in heme biosynthesis.