Activators & Inhibitors

16-phenoxy tetranor Prostaglandin F2α isopropyl ester (Legacy Tebubio ref. 282T37936). Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Stable, lipophilic analogs of PGF2α are used to modulate luteolysis and treat glaucoma. 16-phenoxy tetranor Prostaglandin F2α isopropyl ester (16-phenoxy tetranor PGF2α isopropyl ester) is a lipophilic analog of 16-phenoxy tetranor PGF2α. Isopropyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.

16-phenoxy tetranor Prostaglandin F2α methyl ester (Legacy Tebubio ref. 282T37937). Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Stable, lipophilic analogs of PGF2α are used to modulate luteolysis and treat glaucoma. 16-phenoxy tetranor Prostaglandin F2α (16-phenoxy tetranor PGF2α) is a metabolically stable form of PGF2α containing a 16-phenoxy group at the ω-terminus. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α. 16-phenoxy tetranor PGF2α methyl ester is a lipophilic analog of 16-phenoxy tetranor PGF2α. Methyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.

17-phenoxy trinor Prostaglandin F2α ethyl amide (Legacy Tebubio ref. 282T37938). Prostaglandin F2α (PGF2α), acting through the FP receptor, causes smooth muscle contraction and exhibits potent luteolytic activity. Both 17-phenyl trinor PGF2α and 16-phenoxy tetranor PGF2α are metabolically stable analogs of PGF2α and potent agonists for the FP receptor. 17-phenoxy trinor PGF2α ethyl amide is a lipophilic analog of 17-phenoxy trinor PGF2α . Ethyl amides of PGs serve as prodrugs, as they are hydrolyzed in certain tissues to generate the bioactive free acid.

N-Desethyl Bimatoprost (Legacy Tebubio ref. 282T37939). N-Desethyl Bimatoprost (17-phenyl trinor PGF2α amide) is an F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative PG hypotensive prodrugs. Although it has been claimed that PG amides are not converted to the free acids in vivo, studies have shown that bovine and human corneal tissue converts the amides of various PGs to the free acids with a conversion efficiency of about 10-20% relative to the hydrolysis of isopropyl esters. 17-phenyl trinor PGF2α amide would be expected to show the typical intraocular effects of latanoprost, but with the much slower hydrolysis pharmacokinetics of the PG N-amides.

Pentagalloylglucose (Legacy Tebubio ref. 282T3794). 1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO)/cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg/ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 micro

17-phenyl trinor Prostaglandin F2α cyclopropyl amide (Legacy Tebubio ref. 282T37940). 17-phenyl trinor Prostaglandin F2α cyclopropyl amide (17-phenyl trinor PGF2α cyclopropyl amide) is a novel analog of 17-phenyl trinor PGF2α ethyl amide. There are no published reports on the biological activity of 17-phenyl trinor PGF2α cyclopropyl amide.

17-phenyl trinor Prostaglandin F2α cyclopropyl methyl amide (Legacy Tebubio ref. 282T37941). Prostaglandin F2α (PGF2α) activates the FP receptor, promoting smooth muscle contraction and luteolysis. 17-phenyl trinor PGF2α binds the FP receptor on ovine luteal cells with a relative potency of 756% compared to that of PGF2α. It is produced in vivo by the hydrolysis of 17-phenyl trinor PGF2α ethyl amide. 17-phenyl trinor PGF2α ethyl amide is used to reduce intraocular pressure related to glaucoma. 17-phenyl trinor PGF2α cyclopropyl methyl amide is a lipophilic analog of 17-phenyl trinor PGF2α. Amides of PGs may serve as prodrugs, as they are hydrolyzed in certain tissues to generate the bioactive free acid.

17-phenyl trinor Prostaglandin F2α dimethyl amide (Legacy Tebubio ref. 282T37942). 17-phenyl trinor Prostaglandin F2αdimethyl amide is an isomer of 17-phenyl trinor prostaglandin F2αethyl amide.

17-phenyl trinor Prostaglandin F2α isopropyl ester (Legacy Tebubio ref. 282T37943). 17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog approved as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost. The N-ethyl amide prostaglandin prodrugs are converted into the active free acid more slowly than analogous prostaglandin ester prodrugs like latanoprost. This product is the isopropyl ester of the free acid prostaglandin corresponding to Bimatoprost. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist, and in human and animal glaucoma models, FP receptor agonist activity closely correlates with intraocular hypotensive activity. The 17-phenyl trinor PGF2α isopropyl ester derivative was examined for IOP-lowering activity during latanoprost's development and, at a dose of 3 μg/eye in monkeys, was the most potent analog, reducing IOP by 1.3 mm Hg more than latanoprost, though it was also significantly more irritating to the eye.