Activators & Inhibitors

A2B receptor antagonist 2 (Legacy Tebubio ref. 282T37793). A2B receptor antagonist 2 is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

Rec 15/2615 (hydrochloride) (Legacy Tebubio ref. 282T37794). Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2

Retrobradykinin (Legacy Tebubio ref. 282T37795). Bradykinin analog nonapeptide. Reverse sequence of Bradykinin. Exhibits no significant kinin activity. Can be used as a negative control.

Voriconazole N-oxide (Legacy Tebubio ref. 282T37796). Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole . It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.

Coumarin-Quinone Conjugate (Legacy Tebubio ref. 282T37797). Coumarin-quinone conjugate is a fluorescent substrate for NADH:ubiquinone oxidoreductases.1It is comprised of a coumarin fluorophore conjugated to a ubiquinone analog that can be reduced by NADH:ubiquinone oxidoreductases. It has been used to measure the kinetic parameters of apoptosis-inducing factor mitochondria-associated 2/ferroptosis suppressor protein 1 (AIFM2/FSP1).

Petromyzonol (Legacy Tebubio ref. 282T37798). Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.[1]

PF 04671536 hydrochloride (Legacy Tebubio ref. 282T37799). Potent and selective PDE8B/8A inhibitor ( IC50 values are 1.3 and 1.9 nM, respectively). Exhibits selectivity for PDE8A/B over other PDEs (IC50 values are >10 μM) and a range of other targets. Increases glucose-dependent insulin secretion from human pacreatic islet cells. Orally bioavailable.

Oroxin B (Legacy Tebubio ref. 282T3780). Oroxin B (Hypocretin-2) has antioxidant activity.

rac-Desethyl Oxybutynin (hydrochloride) (Legacy Tebubio ref. 282T37801). rac-Desethyl oxybutynin is an active metabolite of the muscarinic acetylcholine receptor (mAChR) antagonist oxybutynin .1,2,3rac-Desethyl oxybutynin is formed from oxybutynin by the cytochrome P450 (CYP) isoform CYP3A4.2It binds to mAChRs in isolated rat bladder, submaxillary gland, heart, and colon with Kivalues of 5.38, 3.12, 16, and 5.59 nM, respectively.rac-Desethyl oxybutynin (0.4 and 0.8 mg/kg) reduces micturition pressure in rats.3