arterial hypertension

Pulmonary arterial hypertension agent-1 (example 15), recognized as a click chemistry reagent in [1], includes an Alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with Azide group-containing molecules. This compound is utilized specifically for treating pulmonary arterial hypertension.

Nebentan potassium (YM598) is an orally active and selective nonpeptide endothelin receptor (ETA receptor) antagonist.Nebentan potassium inhibits pulmonary arterial hypertension and may be useful in the study of neurologic and cardiovascular diseases.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

Riociguat (BAY 632521) is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.

Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension.

FUREGRELATE, a thromboxane A2 (TxA2) synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets.

Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.

Traumatic Acid (Dodec-2-Enedioic Acid) is a product of the hydroperoxide lyase pathway in plants. Potential as a wound healing agent that stimulates cell division near a wound site to form a protective callus.

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

MRE-269 (ACT-333679) is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269(ACT-333679) is used for the treatment of pulmonary arterial hypertension. MRE-269(ACT-333679) is an active metabolite of Selexipag (S253150).

Riociguat-13C-d6 is the 13C and deuterated compound of Riociguat. Riociguat has a CAS number of 625115-55-1. Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Sildenafil-d8 is a deuterated compound of Sildenafil. Sildenafil has a CAS number of 139755-83-2. Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor, used to treat erectile dysfunction and reduce symptoms of pulmonary arterial hypertension (PAH).

Quinapril-d5 is intended for use as an internal standard for the quantification of quinapril by GC- or LC-MS. Quinapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor quinaprilat. In vivo, quinapril reduces mean arterial pressure in renal hypertensive and spontaneously hypertensive rats. It inhibits angiotensin I-induced pressor responses in normotensive rats and dogs. Quinapril prevents left ventricular heart failure in CHF 14.6 cardiomyopathic hamsters. Formulations containing quinapril have been used in the treatment of hypertension, heart failure, and diabetic nephropathy.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

Seralutinib (GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.

Sotatercept (ACE-011), a soluble activin receptor type IIA (ACVR2A) IgG Fc fusion protein, aims to rebalance growth-promoting and inhibiting signaling pathways by targeting activin and growth differentiation factors. This compound shows potential in treating pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, and multiple myeloma (MM) osteolytic lesions [1] [2] [3] [4] [5].

BMPR2-IN-1 (Compound 8a), is a potent inhibitor of BMPR2, exhibiting an IC50 value of 506 nM and a Kd of 83.5 nM. It is utilized in the study of various diseases including pulmonary arterial hypertension, Alzheimer's disease, and cancer [1].

Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective antagonist of the RGD peptide, with potential applications in pulmonary arterial hypertension research [1].

QCC-374 is a prostanoid agonist. It potentially for the treatment of pulmonary arterial hypertension.

cis-Tadalafil (cis-IC-351) is a potent PDE5 inhibitor with an IC50 value of 0.09 μM that can be used to study arterial hypertension.

BMS-193884 is an oral endothelin antagonist for the treatment of congestive heart failure (CHF) and pulmonary arterial hypertension.

Sildenafil-13C-d3 the 13C and deuterated compound of Sildenafil. Sildenafil has a CAS number of 139755-83-2. Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor, used to treat erectile dysfunction and reduce symptoms of pulmonary arterial hypertension (PAH).

PBR28, a TSPO modulator, holds potential for preventative research in Pulmonary Arterial Hypertension (PAH) and is instrumental in brain positron emission tomography (PET) imaging studies through its capacity for radioactive labeling to trace the 18 KDa transporter (TSPO) [1].

Iptakalim, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist. Iptakalim is also a K(ir) 6.1/SUR2B activator that can attenuate hypoxia-induced pulmonary arterial hypertension in rats by endothelial function protection.

ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH) research. This compound demonstrates efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

Moexiprilat, an active metabolite of the prodrug moexipril formed through side chain ester hydrolysis in vivo, functions as an angiotensin-converting enzyme (ACE; IC50 = 2.1 nM) inhibitor. At a concentration of 10 nM, it inhibits the proliferation of primary neonatal rat cardiac fibroblasts stimulated by estrone or angiotensin II. Furthermore, when given at a daily dosage of 50 mg/kg, moexiprilat reduces mean arterial blood pressure and elevates levels of atrial natriuretic peptide, an indicator of hypertension, in ovariectomized mice.

Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.

SY-LB-57 is a highly effective agonist of bone morphogenetic protein (BMP) receptor signaling, suitable for studies of conditions such as bone fractures and pulmonary arterial hypertension [1].

Selexipag-d7 is a deuterated compound of Selexipag. Selexipag has a CAS number of 475086-01-2. Selexipag(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH).

Selexipag Active Metabolite-d7 is a deuterated compound of Selexipag Active Metabolite. Selexipag Active Metabolite has a CAS number of 475085-57-5. MRE-269 is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269 is used for the treatment of pulmonary arterial hypertension. MRE-269 is an active metabolite of Selexipag (S253150).

ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH) research. It has demonstrated efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.

Rodatristat ethyl (KAR5585) is a groundbreaking, orally active, and potent inhibitor of tryptophan hydroxylase 1 (TPH1) that significantly reduces 5-hydroxytryptamine (5-HT) levels and decreases pulmonary arterial hypertension (PAH) at low concentrations.

BMS 182874 is an orally effective and highly selective endothelin receptor ETA antagonist with an IC50 value of 0.150 μM for ETA and a Ki value of 0.055 μM for ETA.BMS 182874 is able to reduce arterial pressure in a rat hypertension model induced by Deoxycorticosterone acetate. BMS 182874 was able to reduce Deoxycorticosterone-induced arterial pressure in a rat model of hypertension and can be used to study cardiovascular disease.

RB-005 is a potent sphingosine kinase isoform 1 (SK1) inhibitor, which may serve as therapeutic agent for proliferative diseases, including hypertension. RB-005, (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.

Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that is hydrolysed to the active diacid trandolaprilat.

MIF098, a macrophage migration inhibitory factor (MIF) antagonist, inhibits pulmonary hypertension associated with SLE and the proliferation and migration of pulmonary arterial smooth muscle cells (PASMC). MIF098 may also be used to study idiopathic pulmonary hypertension.

Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most active beta-lactam, with an MIC at which 50% of isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. Cefminox was especially active against Bacteroides fragilis (MIC90, 2.0 microg/ml), Bacteroides thetaiotaomicron (MIC90, 4.0 microg/ml), fusobacteria (MIC90, 1.0 microg/ml), peptostreptococci (MIC90, 2.0 microg/ml), and clostridia, including Clostridium difficile (MIC90, 2.0 microg/ml)[2]. The use of a single preoperative dose of cefminox was similar in efficacy to 3 doses of cefoxitin administered every 4 hours, and that the serum and tissue concentrations attained provide adequate antibiotic coverage[3]. Moreover, cefminox as a dual agonist of IP (Prostacyclin receptor) and PPARγ (peroxisome proliferator-activated receptor-gamma) that significantly inhibits PASMC proliferation by up-regulation of PTEN (phosphatase and tensin homolog) and cAMP ( cyclic adenosine monophosphate), suggesting that it has potential for treatment of PAH(pulmonary arterial hypertension)[4].

Apelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in vitro. Shows positive inotropic an

Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH).