prostacyclin receptor

Girinimbine (Girinimbin) is a carbazole alkaloid isolated from the plants M. koenigii, M. koenigii, and Murraya koenigii. Girinimbine exhibits a wide range of biological effects, including apoptosis, antitrypanosomal, antiplatelet, antimicrobial, anti-inflammatory, antioxidant, and antitumor activities.

BAY 73-1449 is a potent and selective antagonist of the prostacyclin receptor (IC50 < 0.1 nM).

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).

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

Ralinepag (APD811) is a potent, orally bioavailable agonist of non-prostanoid prostacyclin (IP) receptor, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

BMY 45778 is a potent non-prostaglandin-like prostaglandin partial agonist that inhibits platelet aggregation in humans, rabbits, and mice, with IC50s of 35 nM, 136 nM, and 1.3 μm, respectively.BMY 45778 acts by stimulating prostacyclin receptors.

Prednicarbate (Hoe 777) is a Corticosteroid Hormone Receptor Agonist. Prednicarbate has antipruritic, anti-inflammatory, and vasoconstrictive properties. It also decreases the number of circulating lymphocytes by inhibiting the production of vasodilators such as nitric oxide and prostacyclin.

RO3244794 is a selective prostacyclin (IP) receptor antagonist that can be used to study liver injury.

Carbacyclin, a PGI2 analog, is a prostacyclin (PGI2) receptor agonist and vasodilator with potent inhibitory platelet aggregation.

Taprostene sodium acts as a partial agonist of the prostacyclin (IP) receptor in the prostaglandin class. It interacts with Prostaglandin E2 (PGE2), ONO-AE1-259 (a selective EP2 agonist), and acetylcholine. Taprostene sodium offers significant cardioprotective effects.

Carbaprostacyclin-biotin (cPGI-biotin; Carbacyclin-biotin) is a Carbacyclin linked to biotin. Carbacyclin is an analog of PGI2, functioning as a prostacyclin (PGI2) receptor agonist and a vasodilator, effectively inhibiting platelet aggregation.

AFP-07 is a highly selective and potent agonist. It was used for the prostacyclin receptor.

TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells.

Palmitic acid-1-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid (T2908) is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid (T2908) is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6

Prostaglandin F1α (PGF1α) is a lipid mediator and an endogenous metabolite of prostacyclin, primarily metabolised from DGLA via the COX pathway, and can dose-dependently regulate smooth muscle contraction.

Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 |Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

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).

Cicaprost (ZK 96480) is a potent prostacyclin receptor (IP) agonist, inducing artery relaxation through concentration-dependent mechanisms with an EC50 value of 5.8 nM [1].

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].

Selexipag Active Metabolite-D7 is a deuterated compound of Selexipag Active Metabolite. Selexipag Active Metabolite (T3S2007) 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).

Selexipag-D7 is a deuterated compound of Selexipag. Selexipag (T3216) 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).

Prednicarbate (Standard) is the standard substance of Prednicarbate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Prednicarbate (Hoe 777) is a Corticosteroid Hormone Receptor Agonist. Prednicarbate has antipruritic, anti-inflammatory, and vasoconstrictive properties. It also decreases the number of circulating lymphocytes by inhibiting the production of vasodilators such as nitric oxide and prostacyclin.