Prostaglandin Receptor Agonist

Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with K_is of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.

U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of Thromboxane A2 (HY-113350) (TXA2) and acts as a potent TXA2 (TP) agonist. U-46619 also is a RhoA agonist. U-46619 stimulates the activation of RhoA through TXA2 receptor activation.

CP-432 (CP-734432) is a EP4 receptor agonist with an IC₅₀ of 2 nM for human sources, 8 nM for canine sources, and an EC₅₀ of 1 nM for human sources. CP-432 stimulates cAMP production and activates β-lactamase (β-lactamase) activity via the cAMP response element signaling pathway. CP-432 is applicable to research related to glaucoma.

Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.

Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research.

Latanoprost (PHXA41) is a prostaglandin F2α analogue and can be used for glaucoma research. Latanoprost can effectively pass through cornea and be hydrolyzed by esterase to latanoprost acid. latanoprost acid is an F-prostaglandin (FP) receptor agonist, and can effectively reduce intraocular pressure (IOP) by increasing the outflow of aqueous humor through uvea.

Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI₂) receptor (IP receptor).

KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a K_i and an EC₅₀ of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.

L-902688 is a potent, selective and orally active EP4 receptor agonist with a K_i of 0.38 nM and an EC₅₀ of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors.

Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension.

Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.

BW 245C is a prostanoid DP-receptor (DP1) agonist, used to study stroke.

Ricinoleic acid (purity≥99%), a hydroxy fatty acid, is an attractive feedstock for the production of high-performance lubricants, cosmetics, polymers, surfactants, and coatings. Ricinoleic acid is the main active ingredient of Castor oil (HY-107799). Ricinoleic acid is the agonist for prostaglandin EP3 receptor (EP3 receptor) (EC₅₀ in MEG-01 is 0.5 μM), that causes laxative effects and uterine contraction. Ricinoleic acid exhibits antianxiety-like, anti-inflammatory and pro-inflammatory properties.

Omidenepag (UR-7276), a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC₅₀ of 1.1 nM. Omidenepag shows binding affinities (IC₅₀) 10 nM for h-EP2. Omidenepag is used in research on diseases related to intraocular pressure.

Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.

Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP₂ receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma.

Prostaglandin J2 (PGJ2), an endogenous metabolite of Prostaglandin D2 (PGD2; HY-101988), is a potent PGD2 receptor (DP) agonist with K_is of 0.9 nM and 6.6 nM for hDP and hCRTH2, respectively. Prostaglandin J2 stimulates intracellular cyclic AMP production with an EC₅₀ value of 1.2 nM. Prostaglandin J2 induces oxidative stress and neuronal apoptosis. Prostaglandin J2 induces the accumulation/aggregation of ubiquitinated (Ub) proteins. Prostaglandin J2 is highly neurotoxic and potentially contributes to many neurodegenerative conditions, including Alzheimer's (AD) and Parkinson's diseases (PD).

ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig.

Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC₅₀ of 33 nM and a K_i of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling.

Ricinoleic acid (purity≥85%), a hydroxy fatty acid, is an attractive feedstock for the production of high-performance lubricants, cosmetics, polymers, surfactants, and coatings. Ricinoleic acid is the main active ingredient of Castor oil (HY-107799). Ricinoleic acid is the agonist for prostaglandin EP3 receptor (EP3 receptor) (EC₅₀ in MEG-01 is 0.5 μM), that causes laxative effects and uterine contraction. Ricinoleic acid exhibits antianxiety-like, anti-inflammatory and pro-inflammatory properties.