Cardiovascular Disease

S-2E is an orally active and noncompetitive HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. S-2E has an anti-hyperlipidemic action. S-2E has the potential for familial hypercholesterolemia and mixed hyperlipidemia research.

ZM-804 is a cationic α-helix antimicrobial peptide. ZM-804 targets bacterial cell membranes. ZM-804 demonstrates antimicrobial activity and prevents the infection of tomato plants by Pst DC3000. ZM-804 inhibits the growth of B. subtilis and E. coli (the same MICs of 41.10 μg/mL). ZM-804 exhibits low hemolytic activity.

(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker.

Guaietolin is an organic synthesis intermediate. Guaietolin is a marker of hypertension with significant reduced level in plasma metabolites. Guaietolin can be used for synthesis of sulfonamide esters with carbonic anhydrase inhibitory activity. Guaietolin can be used for glaucoma and hypertension research.

Acein-1 is an angiotensin-converting enzyme (ACE) inhibitor with an IC₅₀ of 16 μM against rabbit lung ACE. Acein-1 does not bind to the catalytic site of ACE and cannot be hydrolyzed by ACE. Acein-1 can be used in the research of hypertension.

1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats.

TLR2/1 agonist-1 is a selective agonist of the TLR2/1 heterodimer. TLR2/1 agonist-1 acts as a hematopoietic recovery inducer to accelerate the recovery of peripheral blood cells. TLR2/1 agonist-1 serves as a G-CSF production inducer to increase serum G-CSF levels. TLR2/1 agonist-1 exhibits radioprotective effects in mice exposed to radiation. TLR2/1 agonist-1 can be used in studies related to acute radiation syndrome.

GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC₅₀ of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research. GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC₅₀ values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension.

Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent.

LNO 9 is an orally active LOXL2 inhibitor and NO donor, with an IC₅₀ of 0.17 μM against human LOXL2. LNO 9 competitively binds to the LTQ cofactor of LOXL2 to form an irreversible complex, thereby inhibiting collagen oxidation and abnormal cross-linking. LNO 9 releases nitric oxide (NO) to increase cGMP levels in pulmonary artery smooth muscle cells. LNO 9 inhibits hypoxia-induced collagen modification and possesses vasodilatory activity. LNO 9 ameliorates right ventricular hypertrophy and pulmonary artery medial thickness in rat models induced by hypoxia and Monocrotaline (HY-N0750), and can be used for research on pulmonary hypertension.

LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies.

Gymnopusin is an L-type voltage-dependent calcium channel blocker and vasorelaxant. Gymnopusin inhibits KCl- and Norepinephrine-induced contractility as well as CaCl₂-induced contractions. Gymnopusin induces endothelium-independent relaxation involving the opening of ATP-sensitive and calcium-activated potassium channels. Gymnopusin disrupts membranes through tonoplast lysis, leading to electrolyte leakage, chlorophyll loss, and photobleaching in duckweed. Gymnopusin inhibits radicle elongation in Amaranthus hypochondriacus seedlings and exhibits phytotoxicity against duckweed. Gymnopusin shows moderate cytotoxicity against mammalian cell lines. Gymnopusin can be used for research on hypertension.

BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).

(S)-Alprenolol is a potent and nonselective β-blocker.

Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure.

CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ET_A) with an IC₅₀ value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.

Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC₅₀ of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC₅₀=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease.

Moexipril-d₅ (hydrochloride) is deuterium labeled Moexipril (hydrochloride).

NPRA agonist-11 (Example 161) is an NPRA (NPR1) agonist, with AC₅₀ values of 1.681 μM and 0.989 μM for humans and monkeys, respectively. NPRA agonist-11 can be used in the research of cardiovascular diseases and other disorders.