Activators & Inhibitors

13C6 Glucosylsphingosine (d18:1) (Legacy Tebubio ref. 282T37928). 13C6 Glucosylsphingosine (d18:1) is an isotopically enriched form of 1-β-D-glucosylsphingosine (d18:1) that is intended for use as an internal standard for the quantification of 1-β-D-glucosylsphingosine by GC- or LC-MS. 1-β-D-Glucosylsphingosine is a lysolipid derivative of glucosylcerebroside that decreases activity of glucocerebrosidase in LA-N-2 cells in a dose-dependent manner.

14-dehydro Zymostenol (Legacy Tebubio ref. 282T37929). 14-dehydro Zymostenol is a precursor to cholesterol .1It increases the percentage of myelin basic protein-positive (MBP+) oligodendrocytes formed from oligodendrocyte precursor cells when used at concentrations of 5.8 and 17 μM.2

(20R)-Ginsenoside Rh1 (Legacy Tebubio ref. 282T3793). (20R)-Ginsenoside Rh1 (20(R)-Ginsenoside Rh1) can inhibit the thrombin-induced conversion of fibrinogen to fibrin.

15(R)-17-phenyl trinor Prostaglandin F2α (Legacy Tebubio ref. 282T37930). 17-phenyl trinor Prostaglandin F2α N-ethyl amide (17-phenyl trinor PGF2α) is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name 17-phenyl trinor PGF2α ethyl amide. Investigations in our lab have shown that 17-phenyl trinor PGF2α ethyl amide is converted by an amidase enzymatic activity in the human cornea to yield the corresponding free acid, with a conversion rate of about 25 μg/cornea/24 hours. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist. 15(R)-17-phenyl trinor PGF2α is the 15-epi, or unnatural" isomer of this active free acid metabolite. It has much diminished FP receptor-mediated activity

15(S)-Latanoprost (Legacy Tebubio ref. 282T37931). 15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys. 15(S)-Latanoprost is a potential impurity in most commercial preparations of the latanoprost bulk drug product.

15-keto Latanoprost (Legacy Tebubio ref. 282T37932). Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group without isopropyl ester hydrolysis produces 15-keto latanoprost. 15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type PGs; for example, PGF2α will produce this degree of miosis at a dose of less than 1

15-keto Latanoprost (free acid) (Legacy Tebubio ref. 282T37933). 15-keto Latanoprost is a potential metabolite of latanoprost when administered to animals and is a common minor impurity in commercial preparations of the bulk drug compound. Although much less potent than latanoprost, 15-keto Latanoprost can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure in normal cynomolgus monkeys at a dose of 1 μg/eye. It also acts as a miotic in normal cats, causing an 8 mm Hg reduction in pupillary diameter at 5 μg/eye, though it is not as potent as many other F-type prostaglandins, such as prostaglandin F2α, which achieves the same effect at less than 1 μg/eye.

15-keto-17-phenyl trinor Prostaglandin F2α (Legacy Tebubio ref. 282T37934). Bimatoprost is an F-series prostaglandin (PG) analog approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group and amide hydrolysis of Bimatoprost produces 15-keto-17-phenyl trinor PGF2α, a potential metabolite when administered to animals. 15-keto PG analogs can be minor impurities in commercial preparations of corresponding bulk drug compounds. Although much less potent than the parent compound, 15-keto PGs can still produce a small but measurable decrease (1 mm Hg) in intraocular pressure of normal cynomolgus monkeys at a dose of 1 μg/eye. 15-keto Latanoprost (15-keto-17-phenyl-13,14-dihydro trinor PGF2α isopropyl ester) acts as a miotic in normal cat eyes, causing an 8 mm reduction in pupillary diameter at 5 μg/eye. This is less potent compared to many other F-type PGs; for example, PGF2α induces similar miosis at less than 1 μg/eye.

16-phenoxy tetranor Prostaglandin F2α cyclopropyl methyl amide (Legacy Tebubio ref. 282T37935). The actions of many clinical F-series prostaglandins (PGs), including those used for estrous synchronization and for reduction of intraocular pressure (IOP), are mediated through the PGF2α (FP) receptor. 16-phenoxy tetranor Prostaglandin F2α cyclopropyl methyl amide (16-phenoxy tetranor PGF2α cyclopropyl methyl amide) is an analog of PGF2α containing a 16-phenoxy group on the lower (ω) side chain and a cyclopropyl methyl amide at the C-1 position. There are no published reports on the biological activity of 16-phenoxy tetranor PGF2α cyclopropyl methyl amide.