Activators & Inhibitors

Galanin (Human) (Acetate) (Legacy Tebubio ref. 282T38110). Galanin (Human) (Acetate) is a 30-amino acid neuropeptide and galanin (GAL) receptor agonist.It inhibits forskolin-induced cAMP production in HEK293E cells expressing recombinant human GAL1 receptors (EC50= 0.031 nM) and stimulates inositol phosphate accumulation in CHO cells expressing recombinant human GAL2receptors (EC50= 12.3 nM).Human galanin induces contractions in isolated rat longitudinal fundus strips with an EC50value of 13.8 nM.Intrathecal administration of human galanin (3, 10, and 30 nmol/animal) reduces paw licking and flinching in the second, but not first, phase of the formalin test in rats.

Dimethyl-W84 (dibromide) (Legacy Tebubio ref. 282T38111). Dimethyl-W84 is a selective allosteric modulator of the M2 muscarinic acetylcholine receptor. It hinders the dissociation of the orthosteric antagonist N-methylscopolamine from the M2 receptor with an EC50 value of 3 nM.

DL-Tryptophan octyl ester (hydrochloride) (Legacy Tebubio ref. 282T38112). Tryptophan is an amino acid precursor of serotonin and melatonin. DL-Tryptophan octyl ester is a tryptophan derivative with an octyl ester protected COOH group. This addition creates a stable, cell-permeable molecule capable of generating free tryptophan upon hydrolysis of the ester bond.

AL 6598 (Legacy Tebubio ref. 282T38113). Elevated intraocular pressure (IOP) is an important risk factor in developing glaucoma. Certain prostaglandins such as PGF2α and PGD2, have been shown to reduce IOP. AL 6598 is the isopropyl ester prodrug of AL 6556, a PGD2 receptor agonist that binds to DP receptors with a Ki value of 3.2 μM and demonstrates an EC50 value of 0.80 μM in an in vitro functional assay. Designed to enhance corneal absorption, AL 6598 produces a maximum 53% drop in IOP of the ocular hypertensive monkey with a 1 μg dose given twice daily.

AL 8810 ethyl amide (Legacy Tebubio ref. 282T38114). AL 8810 is an 11β-fluoro analog of prostaglandin F2α (PGF2α) which acts as a potent and selective antagonist at the FP receptor. AL 8810 ethyl amide is an analog of AL 8810 in which the C-1 carboxyl group has been modified to an N-ethyl amide. This modification is analogous to the PG N-ethyl amides, as typified by Bimatoprost, that have been introduced as alternative PG ocular hypotensive prodrugs. In contrast to AL 8810 which contracted the cat iris, AL 8810 ethyl amide showed no contraction activity at concentrations up to 10-4 M and did not antagonize the activity of PGF2α-ethanolamide in this system.

Fluprostenol serinol amide (Legacy Tebubio ref. 282T38115). 2-arachidonyl glycerol (2-AG) exhibits cannabinoid (CB) agonist activity at the CB1 receptor, is an important endogenous monoglyceride species, and is thus considered to be the natural ligand for the CB1 receptor. 2-AG can also be metabolized by cyclooxygenase-2 and specific prostaglandin H2 (PGH2) isomerases to form PG 2-glyceryl esters. Fluprostenol serinol amide (Flu-SA) is a stable analog of PGF2α 2-glyceryl ester that has much greater stability. The biological activity of Flu-SA has not yet been determined.

WSP-5 (Legacy Tebubio ref. 282T38117). WSP-5 (Washington State Probe-5) is a fluorescent probe containing an active disulfide group, used for rapid detection of H2S in biological samples and cells.

Zanamivir-13C,15N2 (Legacy Tebubio ref. 282T38118). Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg/kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza.

(20R)-Ginsenoside Rg3 (Legacy Tebubio ref. 282T3812). (20R)-Ginsenoside Rg3 (20(R)-Propanaxadiol) is a compound with anti-aging and antifatigue activities.