Activators & Inhibitors

GAT229 (Legacy Tebubio ref. 282T38204). GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

3-Aminopropylphosphonic Acid (Legacy Tebubio ref. 282T38205). 3-aminopropylphosphonic acid (3-APPA) is a phosphonic analog of GABA that acts as a partial agonist of GABAB receptors (IC50 = 1.5 μM in a radioligand binding assay).

Paracetamol-cysteine TFA (Legacy Tebubio ref. 282T38206). Paracetamol-cysteine TFA (APAP-Cys TFA) is a metabolite of Paracetamol, a biomarker of paracetamol metabolism.

3-hydroxy Undecanoic Acid (Legacy Tebubio ref. 282T38207). 3-hydroxy Undecanoic acid is a hydroxylated fatty acid that has been found in S. algae, LPS extracted from clinical isolates of B. catarrhalis, and methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by P. flava isolated from oil-contaminated soil. It inhibits sodium current in axons dissected from mantles of giant squid (D. bleekeri) with an ED50 value of 0.46 mM.

Heneicosapentaenoic Acid (Legacy Tebubio ref. 282T38208). Heneicosapentaenoic Acid (HPA) is a 21:5 ω-3 fatty acid present in trace amounts in the green alga *B. pennata* and in fish oils. Its structure is similar to eicosapentaenoic acid (EPA) but elongated with one carbon at the carboxyl end, placing the first double bond in the δ6 position. HPA is utilized to study the significance of the position of double bonds in ω-3 fatty acids and incorporates into phospholipids and triacylglycerol in vivo as efficiently as EPA and docosahexaenoic acid. It strongly inhibits arachidonic acid synthesis from linoleic acid, is a poor substrate for prostaglandin H synthase (PGHS) (cyclooxygenase) and 5-lipoxygenase, but rapidly inactivates PGHS.

Hodgkinsine (Legacy Tebubio ref. 282T38209). Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg.

Deapioplatycodin D (Legacy Tebubio ref. 282T3821). Deapioplatycodin D and platycodin D can regulate the production and secretion of airway mucin and, at least in part, explains the traditional use of aqueous extract of APG as expectorants in diverse inflammatory pulmonary diseases. Deapi-platycodin D has anti-inflammatory activity.

Hodgkinsine B (Legacy Tebubio ref. 282T38210). Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg/kg.

Monogalactosyl Diglyceride (Legacy Tebubio ref. 282T38211). Monogalactosyl diglyceride is a minor galactolipid present in oligodendrocytes and myelin, as well as comprises a major fraction of the lipids in photosynthesizing plants and green microorganisms. [1][2] It is used as a marker for myelination and has also been shown to stimulate PKCα activity in oligodendrocytes. [2]