Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

Plasma kallikrein-IN-1 is a PKK inhibitor with an IC 50 value of 0.5 nM.

Plasma kallikrein-IN-2, a potent inhibitor of plasma kallikrein (PKal) with an inhibitory concentration (IC) 50 value of 0.1 nM, is utilized in research targeting hereditary angioedema, diabetic macular edema, and diabetic retinopathy.

Aristolochic acid B (Aristolochic Acid II) is one of the major components of the carcinogenic plant extract aristolochic acid, is known to be mutagenic and to form DNA adducts in vitro and in vivo, Aristolochic acid B shows more carcinogenic risk than aristolochic acid I, and this may be, at least partly, the result of its increased levels in kidney and plasma.

5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid and a methylated derivate of tetrahydrofolate. It is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid.

Methyl acetylsalicylate (ACETYLSALICYLIC ACID METHYL ESTER) is a natural product isolated from Pisum sativum. Inhibition of collagen-induced human platelet rich plasma aggregation

Cepharanthine (NSC-623442), a biscoclaurine alkaloid, suppresses tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and inhibits cytokine production.

2-(4-Methoxyphenyl)acetic acid, a plasma metabolite, is highly sensitive and specific and can be used as a bioindicator to differentiate non-small cell carcinoma patients from healthy controls.

1-Hydroxyoctadecane (OctadecanolOctadecanol) is a fatty alcohol present in human and is normally incorporated into plasmalogen lipids. Sjogren-Larsson syndrome is defined by the triad of ichthyosis, mental retardation, and spasticity, and patients accumulate fatty alcohols such as Octadenol in the plasma and cultured fibroblasts.

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.

1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

Oleoylestrone (MP-101) is present in plasma and adipose tissue, has potential antioxidant effects, induces loss of body fat in rats, and can be used for weight loss.

Kinetensin acetate(103131-69-7 free base) is isolated from pepsin-treated human plasma. Kinetensin acetate(103131-69-7 free base) is a neurotensin-like peptide.

RFRP-1 (human) acetate is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, eject

Neuropeptide SF (human) aceate is a neuropeptide that augmented paraventricular CRH release and increased ACTH and corticosterone levels in the plasma.

Caloxin 2A1 acetate is an inhibitor of extracellular plasma membrane Ca2+-ATPase (PMCA) peptide. Caloxin 2A1 acetate inhibits Ca2+-dependent formation of the 140-kDa acid-stable acylphosphate.

Katacalcin acetate(85916-47-8 free base) (PDN 21 acetate) is a potent plasma calcium-lowering peptide.

Somatostatin 1-28 acetate circulates in human plasma. Approximately 46% of the total somatostatin-like immunoreactivity in plasma is due to Somatostatin 1-28 acetate.

FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells.

9-Oxononanoic Acid is an oxidized fatty acid, formed by the autoxidation of linoleic acid, which enhances phospholipase A2 (PLA2) activity and increases the production of thromboxane B2 in isolated human plasma.9-Oxononanoic Acid reduces hepatic neofatty acid synthesis and enhances the activity of rat hepatic carnitine palmitoyltransferase, a marker of β-oxidation. Activity.

C-Reactive Protein (CRP) 77-82 acetate is the 77-82 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis.C-reactive protein (CRP) is an annular (ring

Ono-3307 mesylate is a protease inhibitor with inhibitory effects on a variety of proteases.Ono-3307 mesylate has significant protective effects against liver injury in rats and inhibits the deposition of radiofibrillar proteins in the kidneys and lungs.PF-184298 is a protease inhibitor with potential antioxidant effects in plasma and adipose tissue.PF-184298 can be used in the study of pancreatitis.

Niceritrol (Cardiolipol) is a niacin ester that reduces cholesterol and triglycerides in total plasma and in the VLD and LD lipoprotein fractions.

Z-Gly-Gly-Arg-AMC TFA (66216-78-2 free base) is a thrombin-specific fluorogenic substrate for testing thrombin generation in PRP and platelet-poor plasma (PPP).

Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor that promotes cystic fibrosis transmembrane conductance regulator (CFTR) maturation and plasma membrane stabilization.Cavosonstat is a CFTR stabilizer and can be used to study cystic fibrosis.

JNJ-54717793 is an orally active, brain-penetrating compound that acts as a selective and high-affinity antagonist of the orexin-1 receptor (OX1R) with a plasma EC50 of 85 ng/mL. It demonstrates K_i values of 16 nM for hOX1R (human OX1R) and 700 nM for hOX2R, indicating its strong preference for hOX1R over hOX2R. JNJ-54717793 is recognized for its effectiveness in the treatment of anxiety disorders.

TMP-153 is a novel and potent ACAT inhibitor with an IC50 value of 5-10 nM for intestinal and hepatic ACAT in animals.TMP-153 has a hypocholesterolemic effect, inhibiting cholesterol uptake and lowering plasma cholesterol in rats and hamsters.

Autotaxin-IN-3 is an inhibitor of Autotaxin (IC50 = 2.4 nM) which is responsible for the increase in lysophosphatidic acid in ascites and plasma.

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones. BD-AcAc 2 can elevate plasma levels of acetoacetate and β-hydroxybutyrate, blood Na+, blood glucose levels and blood creatinine levels after oral administration in mice. BD-AcAc 2 can partly prevent muscle weakness in septic mice. BD-AcAc 2 exhibits potential to improve endurance and exercise performance in animal body. BD-AcAc 2 can also be used to research diabetes or Parkinson’s disease.

JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.

MPO-IN-1 is a powerful and orally bioavailable indole-containing inhibitor that acts irrevocably on myeloperoxidase (MPO). With IC50 values of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively, MPO-IN-1 effectively inhibits both enzymes. Furthermore, it exhibits remarkable MPO inhibitory activity in an acute inflammation mouse model.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.

Estramustine (LEO-275) is a nitrogen mustard linked to estradiol, usually as phosphate. Estramustine has been used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.

Sphingomyelins are complex membrane lipids composed of phosphorylcholine, sphingosine, and an acylated group, such as a fatty acid. Lysosphingomyelin is a naturally-occurring lipid which is produced by the removal of the acylated group of sphingomyelin by a deacylase. Lysosphingomyelin may, in turn, serve as a substrate for autotaxin, which removes choline to produce sphingosine-1-phosphate. The receptors and signaling pathways that are activated by lyso-sphingosine are diverse and vary between cell types. Lysosphingomyelin occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases, including dermatitis and Niemann-Pick disease.

DL-Homocysteine thiolactone hydrochloride (DL-Homocysteinethiolactone hydrochloride) is a cysteine derivative that binds to and induces conformational changes in various plasma proteins, slowing coagulation and inducing oxidative stress. It decreases left ventricular systolic blood pressure and cardiac force and induces seizures in vivo.

Tripalmitolein is a triacylglycerol that contains palmitoleic acid at the sn-1, sn-2, and sn-3 positions. It reduces red blood cell deformability in a concentration-dependent manner in a Reid's filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in the JAK2L mouse model of hepatic steatosis. Tripalmitolein plasma levels are decreased in renal patients before dialysis.

(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance, increases fatty acid uptake into brown adipocytes, and decreases serum triglyceride levels in mice. Levels are also elevated in bronchoalveolar lavage fluid (BALF) in humans following exposure to biodiesel exhaust and in exhaled breath condensate in patients with allergic asthma following allergen exposure.[5] [6] Plasma levels of 12(13)-DiHOME are increased immediately following moderate-intensity exercise in mice and humans, an effect that can be prevented by brown adipose tissue removal in the mouse.[7]

XY-52 (Compound 32), an ST2 (Stimulation-2) inhibitor, exhibits IC50 values of 5.68 μM and 4.59 μM in the AlphaLISA and HEK-Blue assays, respectively. It promotes proinflammatory T-cell proliferation and diminishes plasma sST2 and IFNγ biomarkers in a graft versus host disease (GVHD) mouse model [1].

Mitochondria Modulator-1, a mitochondrial regulator, enhances ATP production in mitochondria. It exhibits good oral bioavailability and blood-brain barrier permeability, along with robust plasma stability, showing promise for the investigation of mitochondrial diseases [1].

Celangulin, an insecticidal component derived from Celastrus angulatus, functions by activating calcium channels on the plasma membrane, which leads to an increase in intracellular Ca2+ due to influx from the external environment. Additionally, Celangulin stimulates calcium channels in the endoplasmic reticulum (ER) [1].

C22 Glucosylceramide (d18:1/22:0) is an endogenous glucosylceramide. Glucosylceramides are major constituents of skin lipid membranes where they play a role in maintaining the water permeability barrier. They are precursors in the synthesis of lactosylceramide , as well as oligoglycolipids and gangliosides. Phospholipase A2 (PLA2) type XIIA knockdown increases C22 glucosylceramide (d18:1/22:0) expression in rat brain. It is also increased in the brain, but not the liver or spinal cord, of mice fed a methionine-restricted diet. In human athletes, plasma levels of C22 glucosylceramide (d18:1/22:0) increase during exercise and return to basal levels during recovery. This product contains C22 glucosylceramide (d18:1/22:0) isolated from bovine buttermilk.

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

Syringomycin E, an antifungal cyclic lipodepsinonapeptide, inhibits the growth of Saccharomyces cerevisiae by interacting with the plasma membrane. It induces K+ efflux, Ca2+ influx, and alterations in membrane potential, associated with channel formation [1] [2].

β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.

Olmesartan medoxomil impurity C is an impurity of Olmesartan medoxomil, a potent and selective angiotensin AT1 receptor inhibitor with an IC50 of 66.2 μM.

Picloxydine is a heterocyclic biguanide with antiplaque and antibacterial activity.

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

Nitrated unsaturated fatty acids, such as 10- and 12-nitrolinoleate , cholesteryl nitrolinoleate, and nitrohydroxylinoleate, represent a new class of endogenous lipid-derived signalling molecules. LNO2 isomers serve as potent endogenous ligands for PPARγ and can also decompose or be metabolized to release nitric oxide. 9-Nitrooleate is one of two regioisomers of nitrooleate, the other being 10-nitrooleate (OA-NO2; used for the mixture of isomers), which are formed by nitration of oleic acid in approximately equal proportions in vivo. Peroxynitrite, acidified nitrite, and myeloperoxidase in the presence of H2O2 and nitrite, all mediate the nitration of oleic acid. OA-NO2 is found in human plasma as the free acid and esterified in phospholipids at concentrations of 619 ± 52 nM and 302 ± 369 nM, respectively. OA-NO2 activates PPARγ approximately 7-fold at a concentration of 1 μM and effectively promotes differentiation 3T3-L1 preadipocytes to adipocytes at 3 μM.

Bilirubin conjugate is a stable, water-soluble ditaurate derivative of bilirubin meant to mimic endogenous bilirubin glucuronide derivatives. In vivo, bilirubin circulates in the plasma and is taken up by hepatocytes and conjugated to one or two glucuronic acids in a reaction catalyzed by UDP glucuronidase to form bilirubin mono or diglucuronide. This water-soluble form is then excreted from the liver in bile in the feces or is converted to urobilinogen and excreted in the urine. In addition to aiding in the disposal of heme, bilirubin and its conjugated derivatives have been shown to exhibit anti-oxidant and antimutagenic effects and to play a role in gut barrier function.