endogenously

NCGC00229600 is an allosteric inverse thyrotropin receptor (TSHR) agonist. NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously and can be used in Graves' disease studies.

Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) is a nutritional supplement composed of the hydrochloride salt form of the acetylated form of the endogenously produced L-carnitine, with potential neuroprotective, cognitive-enhancing, anti-depressive and immunomodulating activities. It may also relieve peripheral neuropathy induced by chemotherapy, diabetes or other diseases. In addition, acetyl-L-carnitine may modulate the immune response by increasing T-lymphocytes maturation and may downregulate pro-inflammatory cytokines in response to viruses, such as SARS-CoV-2. It may also disrupt the ACE2 signaling pathway and inhibit the production of reactive oxygen species (ROS).

(R)-pyrrolidine-2-carboxylic acid (D-Proline) is an isomer of the naturally occurring amino acid L-Proline. D-amino acids, including D-Proline, are found in relatively high abundance in human plasma and saliva, potentially originating from bacterial sources or endogenous production via amino acid racemase activity.

Isethionic acid sodium salt (Sodium isethionate) is an organosulfur compound containing a short chain alkane sulfonate linked to a hydroxyl group. Mammals are able to endogenously synthesize Isethionic acid sodium salt via taurine through a possible enzymatic deamination process. Isethionic acid sodium salt can be found in both human plasma and urine. Higher plasma levels of Isethionic acid sodium salt have been shown to be protective against type 2 diabetes.

Palmitoylethanolamide (Impulsin) is an endogenously fatty acid amide. It has a role as an anti-inflammatory drug, an antihypertensive agent, a neuroprotective agent and an anticonvulsant.Upon administration, palmitoylethanolamide may inhibit the release of pro-inflammatory mediators from activated mast cells.

β-Hydroxybutyrate phenylalanine (BHB-Phe) is a ketone body metabolite resulting from the conjugation of β-hydroxybutyrate (BHB) with the essential amino acid L-phenylalanine. It is synthesized endogenously by cytosolic non-specific dipeptidase 2 (CNDP2) in the process of ketogenesis. In diet-induced obese (DIO) mice, a daily dose of BHB-Phe (50 mg/kg) leads to a reduction in food intake, body weight, and the respiratory exchange ratio (RER) without altering activity, oxygen consumption (VO2), or carbon dioxide production (VCO2).

NCG21 is a GPR120 agonist, which showed potent extracellular signal-regulated kinase (ERK) activation in a cloned GPR120 system. NCG21 potently activated ERK, intracellular calcium responses and GLP-1 secretion in murine enteroendocrine STC-1 cells that e

Gaxilose, also known as 4-Galactosylxylose, a synthetic disaccharide and a substrate of intestinal lactase. Gaxilose is used in a new noninvasive diagnostic test based on urine or serum measurement of D-xylose after lactase cleavage of orally administered

Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 μM, respectively) but not measles virus or influenza virus (IC50s = >20 μM for both).3

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]

A6770 is an inhibitor of sphingosine-1-phosphate (S1P) lyase.1It induces accumulation of [3H]sphinganine-1-phosphate ([3H]dhS1P), an S1P lyase substrate, in IT-79MTNC3 cells that endogenously express high levels of S1P lyase (EC50= <0.01 μM), an effect that is reduced in the presence of vitamin B6(EC50= <100 μM). 1.Ohtoyo, M., Tamura, M., Machinaga, N., et al.Scintillation proximity assay to detect the changes in cellular dihydrosphingosine 1-phosphate levelsLipids51(10)1207-1216(2016)

Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Sianati, S., Yousuf, A., et al.A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptorProc. Natl. Acad. Sci. USA116(44)22353-22358(2019)

The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 μg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 μM).

DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.

Resolvin D5 is an oxidised lipid mediator derived from docosahexaenoic acid (DHA) with anti-inflammatory properties. It inhibits the production of interleukin-6 (IL-6) and chemokine CCL5 in LPS-stimulated THP-1 cells via the ERK-NF-κB signalling pathway.

17-oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-Docosahexaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DHA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

Linaprazan glurate inhibits both exogenously and endogenously stimulated gastric acid secretion and can be utilized in studies on gastrointestinal inflammatory diseases and peptic ulcer diseases.

5-aminovalerate (or 5-aminopentanoic acid) is a lysine degradation product. It can be produced both endogenously or through bacterial catabolism of lysine. 5-aminovalerate is formed via the following multi-step reaction: L-lysine leads to cadverine leads

Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously express COX-2. Lornoxicam reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays with IC50 values of 65 and 54 µM, respectively. It reduces carrageenan-induced paw edema in rats when administered intravenously at doses ranging from 0.1 to 9 mg kg. Formulations containing lornoxicam have been used in the management of postoperative pain.

Anabasine ((S)-Anabasine) is an alkaloid extracted from tobacco, acting as a full agonist of nicotinic acetylcholine receptors (nAChRs) with insecticidal activity. It depolarizes TE671 cells that endogenously express human myotypic nAChRs.

CDN-A, a cyclic di-nucleotide, serves as a precursor for synthesizing antibody-drug conjugates (ADC) and acts as a potent stimulator of both innate and adaptive immune responses. In humans, these cyclic di-nucleotides, produced endogenously in response to foreign DNA or by bacterial pathogens, activate the innate immune system by inducing the expression of interferon genes [1] [2] [3].

N-Acylethanolamines (NAEs) are lipid-derived signaling compounds, with arachidonoyl ethanolamide functioning as an endogenous cannabinoid (CB) that activates CB1 and CB2 receptors. Among these, Palmitoleoyl Ethanolamide (POEA) is synthesized endogenously from palmitoleic acid. Notably, unlike arachidonoyl ethanolamide and palmitoyl ethanolamide, POEA lacks antinociceptive effects in the formalin-evoked pain model.

Somatostatin acetate is an endogenously secreted inhibitor of cell proliferation with potential antitumor activity for the study of cancer and neurological disorders.