From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
Plasma kallikrein-IN-3 is a plasma kallikrein inhibitor (IC50: 0.15 μM). Plasma kallikrein-IN-3 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research .
Plasma kallikrein-IN-2 (Compound 198) is a potent plasma kallikrein (PKal) inhibitor with an IC50 of 0.1 nM. Plasma kallikrein-IN-2 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research .
Plasminogen, Human plasma is a secreted protein that upon cleavage by urokinase plasminogen activator (uPA) or tissue plasminogen activator (tPA) is converted to plasmin, a broad range protease capable of cleaving fibrin and other ECM components. Plasminogen also is a proinflammatory regulator that accelerates the healing of acute and diabetic wounds. Plasminogen can be used in studies of wound healing, inflammation and hypoplasminogenemia .
Recombinant Human Serum Albumin (rHSA) is an active compound and possesses an identical conformation to plasma derived HSA. Recombinant Human Serum Albumin (rHSA) has no difference between rHSA and plasma derived HSA. Recombinant Human Serum Albumin (rHSA) has high efficacy of rHSA with little or no adverse reaction .
Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI50 value of 6.96 and Ki value of 2.4 nM for human plasma cholinesterase (ChE) .
(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. (Rac)-Idroxioleic acid has anti-tumor effect .
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine. Clomipramine is a tricyclic antidepressant .
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
cPcAMP1/26 is an antimicrobial peptide. cPcAMP1/26 effectively kills A.hydrophila and S. aureus. cPcAMP1/26 induces depolarization of the bacterial plasma membrane, and increases intracellular ROS levels .
Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine[1]
Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers .
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models .
Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasma membrane. Zymosterol circulates within the cell .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
PPACK is a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK also inhibits the binding of rt-PA to plasma protease inhibitors .
CB1 antagonist 4 is a inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. CB1 antagonist 4 can reduce body weight, improve plasma inflammatory markers and glucose homeostasis .
1,2-DImyristoyl-rac-glycero-3-phosphocholine (DMPC), a zwitterionic phospholipid, is chosen as a simple eukaryotic cell membrane, mimicking the neutral charge of the surface membrane of eukaryotic plasma membranes .
PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system .
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds .
sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML) .
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes .
Mem-C1C18 is a polarity-sensitive fluorescent probe with excellent plasma membrane anchoring, high brightness and a sensitive response to environmental polarity by altering the fluorescence lifetime. Mem-C1C18 can be used to quantify changes in the polarity of the plasma membrane during iron death .
Monoamine oxidase (EC 1.4.3.4) is an enzyme composed of different polypeptides. Monoamine oxidation catalyzes the oxidative deamination of various biological amines in brain and peripheral tissues by producing hydrogen peroxide. Monoamine oxidase plays an important role in maintaining the regulation of synaptic transmission, emotional behavior and other brain functions .
C6 NBD Sphingomyelin is a fluorescent short-chain analogue of Sphingomyelin (HY-113498). Chlamydia trachomatis acquires C6 NBD Sphingomyelin endogenously synthesizes from C6-NBD-ceramide and transportes to the chlamydial inclusion. C6 NBD Sphingomyelin can incorporate into the plasma membrane .
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer .
Antifungal agent 38 is a geterocyclic disulfide, an antifungal and antibacterial agent. Antifungal agent 38 induces the shrinkage of hyphae, disrupts the integrity of the plasma membrane, and causes the damage and leakage of cell contents .
Antimicrobial agent-24 (compound E8) is a hydrazide compound with excellent and broad-spectrum fungicidal activities. Antimicrobial agent-24 affects the normal function of the plasma membrane, further generating changes in the morphology and subcellular structure of mycelia .
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .
[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa .
Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important drug for African trypanosomiasis. Melarsoprol is also active against leukemia cell lines and plasma cells from myeloma patients. Melarsoprol increases the biliary output of GSH in rats .
Ubretid is a potent inhibitor of plasma cholinesterase. Ubretid therefore delays the hydrolysis of suxamethonium and prolongs its action, similar to the effects shown by other anticholinesterase agents, such as pyridostigmine and donepezil. Ubretid has the potential for the research of urinary retention prolongs the effect of suxamethonium. Ubretid is commonly prescribed for the research of myasthenia gravis and for difficulty in emptying the bladder .
ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
Luvadaxistat (TAK-831) is an orally active, highly selective, potent D-amino acid oxidase (DAAO) inhibitor. Luvadaxistat inhibits oxidative deamination of D-serine via the human recombinant DAAO enzyme with an IC50 of 14 nM. Luvadaxistat significantly increases D-serine levels in the rodent brain, plasma, and cerebrospinal fluid. Luvadaxistat has the potential for schizophrenia research .
SARS-CoV-2 nsp14-IN-2 is a potent SARS-CoV-2 Nsp14 methyltransferase inhibitor with an IC50 value of 0.093 µM. SARS-CoV-2 nsp14-IN-2 shows antiviral activity. SARS-CoV-2 nsp14-IN-2 shows plasma and liver S9 stability. SARS-CoV-2 nsp14-IN-2 has the potential for the research of COVID-19 .
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
FR-167356 is a potent, orally active and selective vacuolar ATPase inhibitor with IC50 values of 170, 220, 370, and 1200 nM for osteoclast plasma membranes, macrophage microsomes, renal brush border membranes, and liver lysosomal membranes, respectively. FR-167356 inhibits bone resorption and ovariectomy-induced bone loss .
YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
Hylambatin, a tachykinin, increases both plasma glucose and plasma insulin, whereas the secretion of glucagon was not affected. Hylambatin can be used in diabetes research .
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
Hexanoylcarnitine exists in human urine and plasma. Hexanoylcarnitine can be used as a plasma detection indicator in patients with methylmalonic aciduria, propionic acidemia, and medium-chain acyl-CoA dehydrogenase deficiency .
GRPP (human) is a 30 amino acid Gcg-derived peptide. GRPP (human) causes slight increases in plasma insulin and decreases in plasma glucagon. GRPP (human) does not affect insulin secretion in rat islets .
Polydextrose has the effect of lowering cholesterol and plasma lipids, and can effectively reduce low-density lipoprotein cholesterol. Polydextrose significantly reduced plasma and liver cholesterol in gerbils fed with enlarged endogenous cholesterol reservoirs .
Teneligliptin hydrobromide hydrate is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
3-Methylsalicylic acid is a salicylic acid derivative that acts on human plasma and has significant fibrinolytic activity by activating the fibrinolytic system.
Butyrylcarnitine is a metabolite in plasma, acts as a biomarker to improve the diagnosis and prognosis of heart failure, and is indicative of anomalous lipid and energy metabolism.
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively .
Linalool (Standard) is the analytical standard of Linalool. This product is intended for research and analytical applications. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity .Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome .
L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a noncompetitive manner and suppresses the plasma glucose increase due to sucrose ingestion.
Linalool-d3 is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].
2-(4-Methoxyphenyl)acetic acid is a plasma metabolite, with high sensitivity and specificity value as a biomarker for discriminating between NSCLC and healthy controls.
Vertilmicin sulfate combines with FMOC-Cl to form the Vertilmicin-FMOC-Cl adduct, and can be used for the determination of glucosamine sulfate in plasma .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
Kallikrein, Porcine pancreas (kininogenase) is capable of forming the kallikrenase kalinin system (KKS) in plasma and tissues, producing bradykinin and kalin peptides, respectively .
Glycochenodeoxycholic acid 3-glucuronide is a type of steroid glucuronide and a plasma metabolite that can be used for biomarker research in diabetes and hepatocellular carcinoma (HCC) .
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .
Menbutone, an oxobutyric acid derivative, is a choleretic with a rapid onset of action, reaching its maximum plasma levels within 1 hour and lasting for approximately 10 hours.
H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
8-Oxoepiberberine is an alkaloid metabolite in the plasma after oral administration of Zuojin formula, a traditional chinese medicine used to treat gastrointestinal disease .
Piperulin A is a potent inhibitor of PAFR. Piperulin A inhibits the specific binding of PAFR on isolated rabbit platelet plasma membranes with an IC50 of 7.3 μM .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasma membrane (PM), causing the plasma membrane to fluoresce .
Lactosylceramide (bovine buttermilk) (LacCer (bovine buttermilk)) is a sphingolipid that highly expressed on the plasma membranes of human phagocytes. Lactosylceramide mediates phagocytosis, chemotaxis, and superoxide generation .
Ezetimibe hydroxy glucuronide (SCH 488128) is a trace metabolite detected in dog and human plasma samples after oral administration of Ezetimibe (HY-17376) .
Ecallantide (DX-88) is a specific plasmakallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema .
Cholesterol-d is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
3-Hydroxyisovalerylcarnitine is a carnitine derivative. 3-Hydroxyisovaleryl carnitine in plasma may serve as a novel biomarker of biotin deficiency in humans, with its concentration increasing with biotin deficiency. Biotin deficiency reduces the activity of biotin-dependent 3-methylcrotonyl-CoA carboxylase, hinders the conversion of 3-methylcrotonyl-CoA into 3-methylglutaconyl-CoA, and impairs the leucine catabolism pathway; resulting in plasma 3-Hydroxyisovalerylcarnitine concentrations rise .
JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats .
AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
Ecallantide (DX-88) TFA is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide may be used to prevent acute attacks of angioedema .
Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasmaDipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasmakallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell .
Heptanoyl-L-carnitine chloride (trans-3,4-methylene-heptanoylcarnitine) is an acylcarnitine. Heptanoyl-L-carnitine chloride causes exercise-induced alterations in the human metabolome in plasma and skeletal muscle tissue .
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
Methyl homoveratrate, a metabolite of RWJ-26240 in vivo, can be identified in plasma, urine and faecal extract. McN5691 (RWJ-26240) is a voltage-sensitive calcium channel blocker .
Nicomol is an orally active hypolipidemic agent that can increase the high density lipoprotein cholesterol (HDL-C) level. Nicomol inhibits the rapid rise of plasma free fatty acids .
1-Palmitoyl-2-[3-(diphenylhexatriene)propanoyl]-sn-phosphatidylcholine is a fluorescent probe with a polar phosphatidylethanolamine head group for the determination of surface lipid oxidation in lipoproteins and plasma .
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasma membrane. lsocryptomerin also shows anticancer and antibacterial activities .
BM 15766 sulfate is an inhibitor of 7-dehydrocholesterol δ7-reductase and reduces plasma cholesterol levels. BM 15766 sulfate is a hypolipidemic agent .
Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats .
Sodium thiocyanate reduces plasma levels of the pro-inflammatory cytokine IL-6, and increases the anti-inflammatory cytokine IL-10 levels. Sodium thiocyanate also significantly reduces of ROS formation .
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes .
800CW maleimide is an infrared dye that can be used for labeling molecules that contain free sulfhydryl (–SH) groups (Ex: 778 nm; Em: 796 nm). 800CW maleimide binds to plasma proteins .
Biotin-DADOO is a biotinylation reagent, which can be used to synthesize a biotin-estradiol conjugate (i.e., biotin-DADOO-estradiol) to develop a direct, broad range enzyme immunoassay to measure plasma estradiol concentrations.
SC-435 is an apical sodium-dependent Bile acid (BA) transporter inhibitor. SC-435 can alter hepatic cholesterol metabolism and lower plasma low-density lipoprotein-cholesterol concentrations .
BTCy is a near-infrared (NIR) fluorescence probe with polarity-responsive and cell plasma membrane-targeting properties. BTCy can be used for in vivo imaging of tumor tissue (λex = 561 nm, λem = 600-700 nm) .
HEC72702 is a potent and orally active hepatitis B virus capsid inhibitor with an EC50 values of 0.039 µM. HEC72702 dose-dependently reduced HBV DNA in both the plasma and livers .
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity .
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy .
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol .
4-Aminohippuric acid-d4 is the deuterium labeled 4-Aminohippuric acid. 4-Aminohippuric acid is a diagnostic agent, useful in medical tests involving the kidney, used in the measurement of renal plasma flow.
L-Alloisoleucine-d10 is the deuterium labeled L-Alloisoleucine. L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
SH-42 is a potent and selective inhibitor of human Δ 24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg) .
Oleamide (Standard) is the analytical standard of Oleamide. This product is intended for research and analytical applications. Oleamide is an endogenous fatty acid amide which can be synthesized de novo in the mammalian nervous system, and has been detected in human plasma.
13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
Tauro-ω-muricholic acid sodium (TωMCA sodium) is a bile acid released by the liver and an analog of tauro-α-muricholic acid. Tauro-ω-muricholic acid sodium is investigated as a potential marker in plasma for early-onset neonatal sepsis (EOS) and cholestasis studies
CP-346086 is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 can lower plasma cholesterol and triglycerides in vivo .
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasma membrane research and drug delivery .
Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively .
N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide .
AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level .
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays .
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent .
Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). Estrone sulfate can be used for the research of breast cancer .
A-71497 is the 3-formyl derivative of the antibiotic Tosufloxacin (HY-B1802). A-71497 can produce high plasma levels of tosufloxacin upon both oral and subcutaneous administration to mice .
AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
N-Desmethyl Clomipramine (hydrochloride) (Standard) is the analytical standard of N-Desmethyl Clomipramine (hydrochloride). This product is intended for research and analytical applications. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine. Clomipramine is a tricyclic antidepressant .
M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6 .
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay .
Hexadecanedioic acid-d28 is the deuterium labeled Hexadecanedioic acid. Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
2-Hydroxy-6-methoxybenzoic acid can be used for the determination of acetylsalicylic acid and its major metabolite, salicylic acid, in animal plasma. 2-Hydroxy-6-methoxybenzoic acid exhibits significant analgesic effects .
Soyasapogenol A, a triterpene compound, isolated from soybean. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model .
CP-346086 dihydrate is a potent and orally active microsomal triglyceride transfer protein (MTP) inhibitor, with an IC50 of 2.0 nM for human and rodent MTP. CP-346086 dihydrate can lower plasma cholesterol and triglycerides in vivo .
H-Abu-OH-d3 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
H-Abu-OH-d2 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
H-Abu-OH-d6 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
BODIPY-cholesterol conjugate-3 (compound 7) is a cholesterol analogue with a fluorescent BODIPY group. BODIPY-cholesterol conjugate-3 can be used to simultaneously visualize multiple cholesterol pools in cells, as it is primarily localized to the plasma membrane .
Monatepil maleate (AJ-2615) is a potent and orally active Ca 2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia .
DAF-FM DA (Diaminofluorescein-FM diacetate) is a fluorescent probe for the detection and bioimaging of nitric oxide (NO). DAF-FM DA spontaneously crosses the plasma membrane and is subsequently cleaved by esterases to generate intracellular DAF-FM (Ex/Em=495/515 nm) .
5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid .
Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus .Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK .Nepodin (Musizin) has antidiabetic and antimalarial activities.
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases .
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively .
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression .
Feniralstat (compound 30), a pyrazole derivative, is a potent kallikrein inhibitor with an IC50 of 6.7 nM for Human plasma kallikrein (pKal). Feniralstat has no inhibition on Human KLKl, Human FXIa, Human Factor Xlla (all IC50>40 μM).
Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouse plasma stability, and no obvious cytotoxicity .
6,9,12,15-Hexadecatetraenoic acid-ethyl ester is an orally active n-1PUFA. 6,9,12,15-Hexadecatetraenoic acid-ethyl ester intake can reduce plasma triglyceride content in mice .
BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability .
PPACK TFA is a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK TFA also inhibits the binding of rt-PA to plasma protease inhibitors .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasma membrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
Zalunfiban (RUC-4) dihydrochloride is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban dihydrochloride can be used for the research of myocardial infarction (MI) .
Zalunfiban (RUC-4) is a potent, selective platelet αIIbβ3 antagonist (IC50=45 nM). Zalunfiban can be used for the research of myocardial infarction (MI) .
FXIa-IN-9 (compound 3f) is a potent and selective FXIa inhibitor. FXIa-IN-9 can bind with FXIa and form hydrogen bond (human FXIa Ki: 0.17 nM, rabbit FXIa Ki: 0.5 nM). FXIa-IN-9 also has anticoagulant activity, and can be used in the research of thromboembolic diseases such as atrial fibrillation, stroke, myocardial infarction, deep vein thrombosis, and pulmonary embolism .
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research .
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .
JTP-103237 is a MGAT2 inhibitor (IC50: 0.019 μM and 6.423 μM for hMGAT2 and hMGAT3 respectively). JTP-103237 modulates fat absorption, decreases plasma glucose levels and prevents diet-induced obesity .
M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasma membrane glutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis .
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 µM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models .
Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) proagent. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST .
Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2 .
2-Methylbutyrylcarnitine is a fatty acid metabolite. 2-Methylbutyrylcarnitine is found mainly in the blood and urine of humans and animals and is produced through the pyruvate carboxylation pathway. 2-Methylbutyrylcarnitine exhibits high level in the plasma of subjects with steatohepatitis (NASH) and can be used as an indicator for the diagnosis of metabolic diseases .
AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic .
MB076 is a novel heterocyclic triazole with improved plasma stability. MB076 inhibits seven different Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with Ki values < 1 μM. MB076 acts synergistically in combination with multiple cephalosporins to restore pBCSK(−) susceptibility .
3-Indolyl-β-D-glucuronide, a chromogenic substrate for β-D-glucuronidase, employs in the detection and enumeration of E. coli, yielding a blue precipitate upon cleavage. 3-Indolyl-β-D-glucuronide in? patients' plasma act as a new indicator of renal failure .
Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment .
AJH-836 is an activator of Munc13-1 and PKC ε/α (Kd: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases .
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing .
Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
AC 187 is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
Sutidiazine (ZY-19489) is an orally active and antimalarial agent. Sutidiazine inhibits parasitemia-induced infection. Sutidiazine shows short half-lives (approximately 7 h) and an exposure effect .
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation .
FP-biotin is a potent organophosphorus toxicant, well-suited for searching for new biomarkers of organophosphorus toxicants exposure. FP-Biotin quantifies FAAH, ABHD6, and MAG-lipase activity. FP-biotin is used for studies with plasma because biotinylated peptides are readily purified by binding to immobilized avidin beads .
Estrone sulfate-d5 (sodium) is the deuterium labeled Estrone sulfate sodium. Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
Estrone sulfate-d4 (sodium) is deuterium labeled Estrone sulfate (sodium). Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity .
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor .
Thiazolyl Blue (MTT) is a cell-permeable and positively charged tetrazolium dye that is used to detect reductive metabolism in cells. Thiazolyl Blue is taken up by cells through the plasma membrane and then reduced to formazan by intracellular NAD (P) H-oxidoreductases. Thiazolyl Blue is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis .
TMA-DPH is a hydrophobic fluorescent membrane probe (Ex=355 nm; Em=430 nm). TMA-DPH is able to anchor on the cell surface and localize to different regions of the phospholipid bilayer. By analyzing the fluorescence polarization values of TMA-DPH in the plasma membrane and membrane substructures, the fluidity of the cell membrane can be determined .
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
BF844 mitigate hearing loss associated with USH3 (usher syndrome type III) mutation CLRN1 (clarin-1) N48K. BF844 induces CLRN1 N48K transportes to the plasma membrane. BF844 shows significantly preserves hearing in vivo .
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research .
VTSEGAGLQLQK- 13C6, 15N2 is the 13C and 15N labeled VTSEGAGLQLQK. VTSEGAGLQLQK is an amino acid sequence in the C-terminal region of recombinant human alpha-acid glucosidase (rhGAA). VTSEGAGLQLQK can be used to bind anti-drug antibodies (ADA) in plasma and quantitatively analyze the therapeutic effect .
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
Ocrelizumab is an anti-CD20 antibody that depletes circulating immature and mature B cells but spares CD20-negative plasma cells. The effector mechanisms of Ocrelizumab are complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Ocrelizumab is the first monoclonal antibody for secondary primary progressive multiple sclerosis (PPMS) .
Ziapin 2 is a molecular optomechanical light transducer. Ziapin 2 is an amphiphilic azobenzene with a strong non-covalent affinity to the plasma membrane. Ziapin 2 can be used to photo-modulate the membrane potential in cells of the Gram-positive bacterium Bacillus subtilis. Ziapin 2 enters the lipid membrane very rapidly (≈ 40 ns) .
VTSEGAGLQLQK- 13C6, 15N2 (TFA) is the 13C- and 15N-labeled VTSEGAGLQLQK. VTSEGAGLQLQK is an amino acid sequence in the C-terminal region of recombinant human alpha-acid glucosidase (rhGAA), which can be used to bind anti-drug antibodies in plasma and quantitatively analyze the therapeutic effect .
13-HPOT, a linolenic fatty acid hydroperoxide, is an antibacterial agent. 13-HPOT has a strong dose response effect on three plant pathogen gram negative bacteria: Pectobacterium carotovorum, Pseudomonas syringae and Xanthomonas translucens. 13-HPOT can interact with the lipid representative of the inner bacterial plasma membrane .
VAP-1-IN-3 (compound 136) is a potent amine oxidase vascular adhesion protein-1 (VAP-1) inhibitor, with an IC50 of 0.13 μM for VAP-1 isolated from bovine plasma. VAP-1-IN-3 can be used for the research of inflammatory .
S-5751 is an orally active prostaglandin DP receptor antagonist. S-5751 inhibits cAMP generation in platelet-rich plasma induced by PGD2 with IC50 0.12 μM. S-5751 has anti-inflammatory activity. S-5751 can be used in asthma research .
13,14-Dihydro-15-keto-PGE1 is an inactive metabolite of PGE1. 13, 14-Dihydro-15-Keto-pGE1 inhibited platelet aggregation in ADP-induced human isolated platelet-rich plasma with IC50 14.8 μg/mL .
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
RFRP-1(human) TFA 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, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively .
SRS16-86 is a potent inhibitor of ferroptosis . SRS16-86 is more stable than more stable to metabolism and plasma than Ferrostatin-1 in vivo. SRS16-86 can be used for renal ischemia-reperfusion injury (IRI) and spinal cord injury (SCI) research .
Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasmarenin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension .
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia .
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells .
TZ4M is a 2,4-thiazolidinedione (TZD)-based anti-ADV agent with neuroprotective effects. TZ4M exhibits AChE inhibition in human plasma. TZ4M improves memory and cognitive impairment in adult rats in a scopolamine (HY-N0296)-induced Alzheimer-type model .
TSLP binder-1 (compound 46) is a bicyclic peptide, which binds to thymic stromal lymphopoietin (TSLP) at the site used by IL-7Rα subunit, shows high affinity for TSLP, with KD of 13 nM. TSLP binder-1 reveals good stability in rat plasma and rat lung S9 fraction .
PAR4 antagonist 1 (Compound 48) is a protease activated receptor 4 (PAR4) antagonist with an IC50 of 1.8 nM. PAR4 antagonist 1 has an IC50 of 2 nM against γ-thrombin-activated PAR4 in platelet-rich plasma (PRP). PAR4 antagonist 1 can be used in antithrombotic research .
Squalene synthase-IN-2 (comppund isomer A-(1S, 3R)-14i) is an orally active squalene synthase inhibitor with IC50 values of 3.4, 99 nM for squalene synthase and cholesterol synthesis, respectively. Squalene synthase-IN-2 reduces plasma cholesterol and triglyceride .
Chlorpyrifos-d10 is the deuterium labeled Chlorpyrifos. Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .
13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice .
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER) . Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein .
L-670596 is an orally active and selective thrombsxane A2 receptor/prostaglandin receptor antagonist. L-670596 inhibits arachidonic acid (HY-109590) and U-44069 induced bronchoconstriction in the guinea pig. L-670596 also inhibits the aggregation of human platelet rich plasma induced by U-44069 .
Fotagliptin is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin displays great security in rat and dog. Fotagliptin can be used for Type 2 diabetes mellitus research .
Fotagliptin benzoate is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin benzoate displays great security in rat and dog. Fotagliptin benzoate can be used for Type 2 diabetes mellitus research .
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo .
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].
Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV .
BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids .
SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
(6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
nSMase2-IN-1 is an orally active Neutral sphingomyelinase 2 (nSMase2) inhibitor with an IC50 value of 0.13 ± 0.06 μM. nSMase2-IN-1 is metabolically stable in liver microsomes and orally available with a favorable brain-to-plasma ratio. nSMase2-IN-1 can be used for nervous system disease research .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC .
ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
T18.3 aptamer sodium is an anticoagulant RNA aptamer targeting FV/Va and eliminates the interaction of FV/FVa with phospholipid membranes. T18.3 aptamer sodium exhibits clinically relevant anticoagulant activity in plasma and whole blood and acts synergistically with low molecular weight heparin. The anticoagulant activity of T18.3 aptamer sodium is effectively and rapidly reversed by protamine sulfate .
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasmaEC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
17-Phenyl-ω-trinor-PGE2 is a PGE2 (HY-101952) analog, which is an agonist for EP1 and EP3 receptor. 17-Phenyl-ω-trinor-PGE2 inhibits the PAF-induced aggregation of human platelet-rich plasma (PRP) and Cicaprost (HY-19583) induced Cyclic AMP (HY-B1511) production .
CLP257 is a selective K +-Cl − cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl − transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
17-Phenyl-18,19,20-trinor-PGD2 (17-Phenyl-PGD2) is an analogue of prostaglandin D2 (PGD2; HY-101988). 17-Phenyl-18,19,20-trinor-PGD2 is a potent inhibitor of platelet aggregation caused by aenosine diphosphate (ADP), with the IC50 of 8.4 μM (PGD2 IC50 = 18.6 nM). 17-Phenyl-18,19,20-trinor-PGD2 is a weak agonist of cyclic AMP accumulation .
T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin . T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively .
Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Dextran (MW 70000) is a complex carbohydrate polymer consisting of glucose molecules linked by glycosidic bonds. Dextran has excellent solubility in water, making it useful as a viscosity modifier or stabilizer in foods, paints and adhesives. In the biomedical field, dextran is often used as a plasma expander because of its ability to increase blood volume when administered intravenously. It can also be modified to create dextran-based drug delivery systems, such as targeted nanoparticles.
Dextran (MW 40000) is a complex carbohydrate polymer consisting of glucose molecules linked by glycosidic bonds. Dextran has excellent solubility in water, making it useful as a viscosity modifier or stabilizer in foods, paints and adhesives. In the biomedical field, dextran is often used as a plasma expander because of its ability to increase blood volume when administered intravenously. It can also be modified to create dextran-based drug delivery systems, such as targeted nanoparticles.
1-Arachidonoyl-sn-glycerol 3-phosphate ammonium (20:4 Lyso PA) is a phospholipid and an LPA derived from arachidonic acid. The concentration of 1-Arachidonoyl-sn-glycerol 3-phosphate ammonium in plasma is significantly correlated with the age of onset of cocaine use and the duration of abstinence. 1-Arachidonoyl-sn-glycerol 3-phosphate ammonium can be used in the research of biomarkers for cocaine use disorder (CUD) .
Bromelain is an anti-inflammatory agent derived from pineapple stem that acts through down-regulation of plasma kininogen, inhibition of Prostaglandin E2 expression, degradation of advanced glycation end product receptors and regulation of angiogenic biomarkers as well as antioxidant action upstream in the COX-pathway . Bromelain exhibits various fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory activities. Bromelain also possesses some anticancerous activities and promotes apoptotic cell death .
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent .
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice .
BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasma protein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasma membranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings .
Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
ALN29882 is a glycerolipid located on the plasma membrane. It consists of two fatty acid chains covalently linked to a single glycerol molecule by means of an ester bond. 18:1 DG has been used as a source of diacylglycerol in the diacylglycerol O-acyltransferase 1 (DGAT1) assay. It is also used as a substrate in the DGAT-1 enzyme assay to evaluate compounds as potential inhibitors of DGAT-1. Suitable for lipoprotein overlay screening assays with the recombinant protein His-AtROP6.
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels .
APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury .
APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base effectively prevents kidney injury .
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research .
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure .
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism .
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55 . ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro .
Methylene Violet 3RAX is a phenazine dye to stain the mitochondria of cells. Methylene Violet 3RAX can change the molecular structure of DNA, undermine the module of DNA, and induce the generation of the reactive singlet oxygen. Methylene Violet 3RAX shows inhibition for human erythrocyte AChE and human plasma BChE with an Kis of 1.58, 0.51 μM, respectively. Methylene Violet 3RAX has the potential for the research of potential photosensitizers for mitochondrial targeting action in PDT (photodynamic therapy) .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasma proteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .
Losartan carboxylic acid-d4 (hydrochloride) is deuterium labeled Losartan Carboxylic Acid. Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor) .
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
(R,R)-BD-AcAc 2 ((R,R)-Ketone Ester), a ketone monoester, can be used as a source of oral nutritional ketones. (R,R)-BD-AcAc 2 can elevate plasma levels of β-hydroxybutyrate and acetoacetate, blood glucose, blood Na + levels and blood creatinine levels after oral administration in mice. (R,R)-BD-AcAc 2 can partly prevent muscle weakness in septic mice. (R,R)-BD-AcAc 2 has potential to improve exercise performance and endurance in animal body. (R,R)-BD-AcAc 2 can also be used to research Parkinson’s disease or diabetes .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models .
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
Pharmacokinetic Analysis ICR Male Mice
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.
MCE offers a unique collection of 128 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules.
There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery.
MCE provides a unique collection of 4627 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.
Extracellular vesicles (EVs) are small membrane binding structures that are released from cells into the surrounding environment and play a crucial role in mediating and regulating intercellular communication related to physiological and pathological processes. EVs are lipid membrane vesicles composed of proteins, lipids, and nucleic acids. EVs can be divided into several types based on their source, such as extracellular vesicles, microcapsules, and apoptotic vesicles. The size range of exosomes is 30-150nm, which are endocrine in multi vesicular endosomes (MVEs); microvesicles (50-1000nm) are secreted directly through extracellular interactions, thereby releasing plasma membrane vesicles. In contrast, apoptotic bodies are usually larger, ranging in size from 1 to 5 μ m. This is generated during programmed cell death. EV plays a crucial role in transmitting information between cells and influencing the behavior and function of receptor cells.
MCE designs a unique collection of 401 small molecules related to extracellular vesicles (EVs). It is a good tool to be used for research on metabolize, cancer and other diseases.
C6 NBD Sphingomyelin is a fluorescent short-chain analogue of Sphingomyelin (HY-113498). Chlamydia trachomatis acquires C6 NBD Sphingomyelin endogenously synthesizes from C6-NBD-ceramide and transportes to the chlamydial inclusion. C6 NBD Sphingomyelin can incorporate into the plasma membrane .
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins .
mgc(3Me)FL is the active fluorescent form of mgc(3Me)FDA (HY-D2300) after hydrolysis in cells. mgc(3Me)FL subcellularly localizes to the Golgi apparatus and is a visualized Golgi probe. mgc(3Me)FL also binds to the outer leaflet of the plasma membrane (PM), causing the plasma membrane to fluoresce .
1-Palmitoyl-2-[3-(diphenylhexatriene)propanoyl]-sn-phosphatidylcholine is a fluorescent probe with a polar phosphatidylethanolamine head group for the determination of surface lipid oxidation in lipoproteins and plasma .
800CW maleimide is an infrared dye that can be used for labeling molecules that contain free sulfhydryl (–SH) groups (Ex: 778 nm; Em: 796 nm). 800CW maleimide binds to plasma proteins .
BODIPY-cholesterol conjugate-3 (compound 7) is a cholesterol analogue with a fluorescent BODIPY group. BODIPY-cholesterol conjugate-3 can be used to simultaneously visualize multiple cholesterol pools in cells, as it is primarily localized to the plasma membrane .
DAF-FM DA (Diaminofluorescein-FM diacetate) is a fluorescent probe for the detection and bioimaging of nitric oxide (NO). DAF-FM DA spontaneously crosses the plasma membrane and is subsequently cleaved by esterases to generate intracellular DAF-FM (Ex/Em=495/515 nm) .
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasma membrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
Thiazolyl Blue (MTT) is a cell-permeable and positively charged tetrazolium dye that is used to detect reductive metabolism in cells. Thiazolyl Blue is taken up by cells through the plasma membrane and then reduced to formazan by intracellular NAD (P) H-oxidoreductases. Thiazolyl Blue is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis .
TMA-DPH is a hydrophobic fluorescent membrane probe (Ex=355 nm; Em=430 nm). TMA-DPH is able to anchor on the cell surface and localize to different regions of the phospholipid bilayer. By analyzing the fluorescence polarization values of TMA-DPH in the plasma membrane and membrane substructures, the fluidity of the cell membrane can be determined .
BODIPY TR methyl ester is a lipophilic GFP Counterstain. BODIPY TR methyl ester dye readily permeates cell membranes and localizes in endomembranous organelles but not localize strongly in plasma membranes. BODIPY TR methyl ester is an excellent red fluorescent vital dye (Ex=568 nm, Em=625 nm), can be used to reveal the location and shapes of cell nuclei, the shapes of cells within embryonic tissues, as well as the bound aries of organ-forming tissues within the whole embryo .
Recombinant Human Serum Albumin (rHSA) is an active compound and possesses an identical conformation to plasma derived HSA. Recombinant Human Serum Albumin (rHSA) has no difference between rHSA and plasma derived HSA. Recombinant Human Serum Albumin (rHSA) has high efficacy of rHSA with little or no adverse reaction .
1,2-DImyristoyl-rac-glycero-3-phosphocholine (DMPC), a zwitterionic phospholipid, is chosen as a simple eukaryotic cell membrane, mimicking the neutral charge of the surface membrane of eukaryotic plasma membranes .
Polydextrose has the effect of lowering cholesterol and plasma lipids, and can effectively reduce low-density lipoprotein cholesterol. Polydextrose significantly reduced plasma and liver cholesterol in gerbils fed with enlarged endogenous cholesterol reservoirs .
Plasmin is an important protease present in blood that degrades many plasma proteins, including fibrin clots. Plasmin can also act as a potent regulator of the immune process and can directly interact with various cell types, including monocytes, macrophages, and dendritic cells .
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Lactosylceramide (bovine buttermilk) (LacCer (bovine buttermilk)) is a sphingolipid that highly expressed on the plasma membranes of human phagocytes. Lactosylceramide mediates phagocytosis, chemotaxis, and superoxide generation .
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
Biotin-DADOO is a biotinylation reagent, which can be used to synthesize a biotin-estradiol conjugate (i.e., biotin-DADOO-estradiol) to develop a direct, broad range enzyme immunoassay to measure plasma estradiol concentrations.
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasma membrane research and drug delivery .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
NTPO trisodium is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO trisodium are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Dextran (MW 70000) is a complex carbohydrate polymer consisting of glucose molecules linked by glycosidic bonds. Dextran has excellent solubility in water, making it useful as a viscosity modifier or stabilizer in foods, paints and adhesives. In the biomedical field, dextran is often used as a plasma expander because of its ability to increase blood volume when administered intravenously. It can also be modified to create dextran-based drug delivery systems, such as targeted nanoparticles.
ALN29882 is a glycerolipid located on the plasma membrane. It consists of two fatty acid chains covalently linked to a single glycerol molecule by means of an ester bond. 18:1 DG has been used as a source of diacylglycerol in the diacylglycerol O-acyltransferase 1 (DGAT1) assay. It is also used as a substrate in the DGAT-1 enzyme assay to evaluate compounds as potential inhibitors of DGAT-1. Suitable for lipoprotein overlay screening assays with the recombinant protein His-AtROP6.
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner .
cPcAMP1/26 is an antimicrobial peptide. cPcAMP1/26 effectively kills A.hydrophila and S. aureus. cPcAMP1/26 induces depolarization of the bacterial plasma membrane, and increases intracellular ROS levels .
Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models .
PPACK is a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK also inhibits the binding of rt-PA to plasma protease inhibitors .
Chromogranin A (324-337), human is a peptide fragment of chromogranin A, it can be isolated from human ileal carcinoid tumor. Chromogranin A is a soluble glycoprotein stored with hormones and neuropeptides in secretory granules of most (neuro)endocrine cells and neurons, and it is also a plasma marker of neuroendocrine tumors .
Bz-Ala-Arg is a dipeptide. Bz-Ala-Arg is also a spectrophotometric substrate (0.4 M pyridine formate, pH 4.25) of human pancreatic carboxypeptidase B and plasma carboxypeptidase N. Bz-Ala-Arg can be used to screen competitive inhibitors of these two enzymes .
[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa .
S-(2-Carboxyethyl)-L-cysteine (S-Carboxyethylcysteine) is a non-protein (modified) sulfur amino acid. S-(2-Carboxyethyl)-L-cysteine is present in Acacia seed. S-(2-Carboxyethyl)-L-cysteine can affect the seed’s protein use in rats. S-(2-Carboxyethyl)-L-cysteine suppresses the methionine-induced growth rate, and has a negative effect on the plasma amino acid levels in rats .
Hylambatin, a tachykinin, increases both plasma glucose and plasma insulin, whereas the secretion of glucagon was not affected. Hylambatin can be used in diabetes research .
GRPP (human) is a 30 amino acid Gcg-derived peptide. GRPP (human) causes slight increases in plasma insulin and decreases in plasma glucagon. GRPP (human) does not affect insulin secretion in rat islets .
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
Ecallantide (DX-88) is a specific plasmakallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema .
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats .
RFRP-3 (rat) is a neuropeptide. RFRP-3 (rat) inhibits gonadotropin secretion, causing a marked increase in ghrelin mRNA and plasma growth hormone levels .
KLA peptide is a biological active peptide. (a cationic amphipathic mitochondrial membrane disrupting peptide that induces programmed cell death by disrupting mitochondrial membrane, but cannot cross the plasma
membrane)
Ecallantide (DX-88) TFA is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide may be used to prevent acute attacks of angioedema .
Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca 2+ pump in liver plasma membranes independently of adenylate cyclase activation .
Antifreeze Polypeptide 6 (winter flounder) is the component 6 of the winter flounder's antifreeze polypeptides. Antifreeze Polypeptide 6 (winter flounder) lowers the plasma freezing point by arresting the growth of ice nuclei .
Pegylated synthetic human c-peptide retains bioactivity comparable to that of natural (i.e. non-polyethylene glycolated) C-peptides and has a prolonged circulating residence time in plasma for use in diabetic peripheral neuropathy studies .
(Arg)9 biotin labeled is a cell-permeable peptide. (Arg)9 biotin labeled can be used for drug delivery. (Arg)9 biotin labeled can traverse the plasma membrane of eukaryotic cells .
Osteocalcin (37-49), human is a peptide fragment of Osteocalcin. Osteocalcin (37-49), human has been used to detecte the intact human osteocalcin in HPLC purified plasma and peritoneal dialysate from patients with terminal renal insufficiency and in extracted human bone .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
AC 187 is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .
Proadrenomedullin (45-92), human, a mid-regional fragment of proadrenomedullin (MR-proADM), comprises amino acids 45–92 of pre-proADM. Proadrenomedullin (45-92), human has a longer half-life, is relatively stable and is produced in equimolar amounts to adrenomedullin (ADM), making it a surrogate for plasma levels of ADM gene products .
VTSEGAGLQLQK- 13C6, 15N2 (TFA) is the 13C- and 15N-labeled VTSEGAGLQLQK. VTSEGAGLQLQK is an amino acid sequence in the C-terminal region of recombinant human alpha-acid glucosidase (rhGAA), which can be used to bind anti-drug antibodies in plasma and quantitatively analyze the therapeutic effect .
RFRP-1(human) TFA 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, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
[D-Pro4,D-Trp7,9] Substance P (4-11) is a potent antagonist of Substance P (HY-P0201). [D-Pro4,D-Trp7,9] Substance P (4-11) decreases plasma aldosterone (ALDO) concentration .
Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
α-Hemolysin (Staphylococcus aureus) is one of the most characteristic virulence factors secreted by Staphylococcus aureus, a polypeptide capable of destroying the host cell plasma membrane. After α-Hemolysin binds to the cell surface, its monomers assemble into a homoheptamer to form a front pore, which then transforms into a mature transmembrane pore water channel, allowing K + and Ca 2+ ion transport, leading to necrotic death of target cells .
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasma protein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)
FRETS-VWF73 is a biological active peptide. (FRETS-VWF73 is a very powerful Fluorescence-Quenching Substrate for the VWF cleaving protease ADAMTS-13. It is commonly used as a useful tool for the rapid measurement of ADAMTS-13 activity in plasma and is a predictive marker for various thrombotic diseases like TPP. Our new substrate FRETS-VWF73 can be easily used with a 96-well format in commercial plate readers.)
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
MCE Exosome Isolation and Purification Kit provides a simple and effective method to isolate and purify intact exosomes from plasma and serum that can be used for electron microscope analysis, NTA analysis, WB, qPCR, etc.
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia .
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a KD value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important drug for African trypanosomiasis. Melarsoprol is also active against leukemia cell lines and plasma cells from myeloma patients. Melarsoprol increases the biliary output of GSH in rats .
Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia .
Ocrelizumab is an anti-CD20 antibody that depletes circulating immature and mature B cells but spares CD20-negative plasma cells. The effector mechanisms of Ocrelizumab are complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Ocrelizumab is the first monoclonal antibody for secondary primary progressive multiple sclerosis (PPMS) .
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia .
Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasma membrane. Zymosterol circulates within the cell .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo . YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent . YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation .
Hexanoylcarnitine exists in human urine and plasma. Hexanoylcarnitine can be used as a plasma detection indicator in patients with methylmalonic aciduria, propionic acidemia, and medium-chain acyl-CoA dehydrogenase deficiency .
3-Methylsalicylic acid is a salicylic acid derivative that acts on human plasma and has significant fibrinolytic activity by activating the fibrinolytic system.
Butyrylcarnitine is a metabolite in plasma, acts as a biomarker to improve the diagnosis and prognosis of heart failure, and is indicative of anomalous lipid and energy metabolism.
Linalool (Standard) is the analytical standard of Linalool. This product is intended for research and analytical applications. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity .Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome .
L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a noncompetitive manner and suppresses the plasma glucose increase due to sucrose ingestion.
2-(4-Methoxyphenyl)acetic acid is a plasma metabolite, with high sensitivity and specificity value as a biomarker for discriminating between NSCLC and healthy controls.
Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
Glycochenodeoxycholic acid 3-glucuronide is a type of steroid glucuronide and a plasma metabolite that can be used for biomarker research in diabetes and hepatocellular carcinoma (HCC) .
H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
8-Oxoepiberberine is an alkaloid metabolite in the plasma after oral administration of Zuojin formula, a traditional chinese medicine used to treat gastrointestinal disease .
Piperulin A is a potent inhibitor of PAFR. Piperulin A inhibits the specific binding of PAFR on isolated rabbit platelet plasma membranes with an IC50 of 7.3 μM .
3-Hydroxyisovalerylcarnitine is a carnitine derivative. 3-Hydroxyisovaleryl carnitine in plasma may serve as a novel biomarker of biotin deficiency in humans, with its concentration increasing with biotin deficiency. Biotin deficiency reduces the activity of biotin-dependent 3-methylcrotonyl-CoA carboxylase, hinders the conversion of 3-methylcrotonyl-CoA into 3-methylglutaconyl-CoA, and impairs the leucine catabolism pathway; resulting in plasma 3-Hydroxyisovalerylcarnitine concentrations rise .
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats .
Cholesterol (Standard) is the analytical standard of Cholesterol. This product is intended for research and analytical applications. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
lsocryptomerin is a membrane-active antifungal compound that can be isolated from Selaginella tamariscina. lsocryptomerin can depolarize fungal plasma membrane. lsocryptomerin also shows anticancer and antibacterial activities .
Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats .
Sodium thiocyanate reduces plasma levels of the pro-inflammatory cytokine IL-6, and increases the anti-inflammatory cytokine IL-10 levels. Sodium thiocyanate also significantly reduces of ROS formation .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Oleamide (Standard) is the analytical standard of Oleamide. This product is intended for research and analytical applications. Oleamide is an endogenous fatty acid amide which can be synthesized de novo in the mammalian nervous system, and has been detected in human plasma.
Thiocholesterol is a member of the class of cholesteric liquid crystals (CLCs) that can be used to synthesis cationic lipid. Thiocholesterol is a stronger stabilizer of silver nanoparticles (SNPs). Thiocholesterol can be used for plasma membrane research and drug delivery .
Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). Estrone sulfate can be used for the research of breast cancer .
2-Hydroxy-6-methoxybenzoic acid can be used for the determination of acetylsalicylic acid and its major metabolite, salicylic acid, in animal plasma. 2-Hydroxy-6-methoxybenzoic acid exhibits significant analgesic effects .
Soyasapogenol A, a triterpene compound, isolated from soybean. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model .
5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid .
Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus .Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK .Nepodin (Musizin) has antidiabetic and antimalarial activities.
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs) .
2-Methylbutyrylcarnitine is a fatty acid metabolite. 2-Methylbutyrylcarnitine is found mainly in the blood and urine of humans and animals and is produced through the pyruvate carboxylation pathway. 2-Methylbutyrylcarnitine exhibits high level in the plasma of subjects with steatohepatitis (NASH) and can be used as an indicator for the diagnosis of metabolic diseases .
Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
3-Indolyl-β-D-glucuronide, a chromogenic substrate for β-D-glucuronidase, employs in the detection and enumeration of E. coli, yielding a blue precipitate upon cleavage. 3-Indolyl-β-D-glucuronide in? patients' plasma act as a new indicator of renal failure .
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice .
Coixol (6-Methoxy-2-benzoxazolinone; 6-MBOA) is a potent and orally active anti-inflammatory agent. Coixol decreases the iNOS protein expression. Coixol inhibits the production of TNF-α, IL-6, and IL-1β. Coixol improves glucose tolerance and plasma insulin. Coixol decreases the blood glucose level .
T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin . T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively .
Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment .
Dextran (MW 40000) is a complex carbohydrate polymer consisting of glucose molecules linked by glycosidic bonds. Dextran has excellent solubility in water, making it useful as a viscosity modifier or stabilizer in foods, paints and adhesives. In the biomedical field, dextran is often used as a plasma expander because of its ability to increase blood volume when administered intravenously. It can also be modified to create dextran-based drug delivery systems, such as targeted nanoparticles.
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism .
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Human (HEK293, His, solution) is the recombinant human-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Human (HEK293, His, solution) is 619 a.a., with molecular weight of 72-80 kDa.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface. It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin. This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes. Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is 619 a.a., with molecular weight of 75-85 kDa.
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Cynomolgus (HEK293, His) is 619 a.a., with molecular weight of 70-90 kDa.
Plasma kallikrein (KLKB1) serves as an enzyme, cleaving Lys-Arg and Arg-Ser bonds to release bradykinin from HMW kininogen. It plays a crucial role in the reciprocal activation of factor XII, especially upon binding to a negatively charged surface. Besides its role in the kinin system, KLKB1 may contribute to the renin-angiotensin system by converting prorenin into renin. Plasma kallikrein/KLKB1 Protein, Human (HEK293, His) is the recombinant human-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Human (HEK293, His) is 619 a.a., with molecular weight of 72-80 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, hFc) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of RBP4 Protein, Human (HEK293, hFc) is 183 a.a., with molecular weight of ~50 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from the liver to peripheral tissues. It binds to all-trans retinol, transferring it to STRA6 for cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further aids STRA6 in retinol transport. RBP4 Protein, Rat (HEK293, His) is the recombinant rat-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Rat (HEK293, His) is 183 a.a., with molecular weight of ~24 kDa.
RBP4 Protein transports retinol in blood plasma, delivering it from liver stores to peripheral tissues. Binding to all-trans retinol, it transfers it to STRA6 for efficient cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further supports STRA6 in retinol transport. RBP4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Mouse (HEK293, His) is 183 a.a., with molecular weight of ~22.8 kDa.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, Fc) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of RBP4 Protein, Canine (HEK293, Fc) is 201 a.a., with molecular weight of ~53 kDa.
RBP4 Protein is a member of the lipocalin family and the major transport protein of the hydrophobic molecule retinol, also known as vitamin A, in the circulation. RBP4 Protein, Canine (HEK293, His) is the recombinant canine-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Canine (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human (HEK293, C-His) is the recombinant human-derived RBP4 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of RBP4 Protein, Human (HEK293, C-His) is 183 a.a., with molecular weight of ~21 kDa.
RBP4 protein acts as a retinol-binding protein, essential for transporting retinol in blood plasma. It facilitates the delivery of retinol from the liver to peripheral tissues and likely transfers bound all-trans retinol to STRA6 for cell membrane transport. Interactions with TTR prevent kidney glomeruli filtration loss. Direct interaction with STRA6 underscores RBP4's role in intricate retinol transport and distribution processes in the body. RBP4 Protein, Human is the recombinant human-derived RBP4 protein, expressed by E. coli , with tag free. The total length of RBP4 Protein, Human is 183 a.a., with molecular weight of ~20.0 kDa.
PGCP is a carboxypeptidase with a potentially critical role in the hydrolysis of circulating peptides. It catalyzes the cleavage of terminally unsubstituted dipeptides, releasing amino acids. PGCP Protein, Mouse (HEK293, His) is the recombinant mouse-derived PGCP protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PGCP Protein, Mouse (HEK293, His) is 452 a.a., with molecular weight of ~60.0 kDa.
RBP4 Protein, a vital retinol transporter in blood plasma, mediates the transfer from liver stores to peripheral tissues. It also enhances retinol transport by interacting with TTR. RBP4 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag. The total length of RBP4 Protein, Cynomolgus (HEK293, His) is 183 a.a., with molecular weight of ~23 kDa.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface. It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin. This highlights the protein's multifaceted role in various physiological processes. Plasma kallikrein/KLKB1 Protein, Rat (P.pastoris, His) is the recombinant rat-derived Plasma kallikrein/KLKB1 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of Plasma kallikrein/KLKB1 Protein, Rat (P.pastoris, His) is 248 a.a., with molecular weight of ~34 kDa.
Serpin G1 protein binds complement and inhibits serine-type endopeptidases. It is located in the extracellular space and is involved in aging. Serpin G1 Protein, Rat (HEK293, His) is the recombinant rat-derived Serpin G1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Serpin G1 Protein, Rat (HEK293, His) is 482 a.a., with molecular weight of ~ 70-95 kDa.
Serpin G1, also known as C1-inhibitor, controls C1 complex activation by forming a proteolytically inactive complex with C1r or C1s proteases. Its interactions regulate physiological pathways like complement activation, blood coagulation, fibrinolysis, and kinin generation. As a potent inhibitor of FXIIa, chymotrypsin, and kallikrein, Serpin G1 binds to E. coli stcE, protecting against complement-mediated lysis, and engages with MASP1, showcasing its intricate involvement in various cellular processes. Serpin G1 Protein, Human (500a.a, HEK293, His) is the recombinant human-derived Serpin G1 protein, expressed by HEK293, with C-10*His labeled tag. The total length of Serpin G1 Protein, Human (500a.a, HEK293, His) is 478 a.a., with molecular weight of ~110 kDa.
Carboxypeptidase B2 Protein, Human (HEK293, His) is an approximately 47.0 kDa human carboxypeptidase B2 with a His-flag. Carboxypeptidase B2 is a enzyme belonging to the peptidase M14 family and hydrolyze C-terminal peptide bonds.
HABP2 is a protein that cleaves the alpha chain of fibrinogen as well as the beta chain between "Lys-53" and "Lys-54" at multiple sites, preventing direct formation of a fibrin clot. It activates coagulation factor VII and converts prourokinase into its active form. HABP2 Protein, Human (HEK293, His) is the recombinant human-derived HABP2 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of HABP2 Protein, Human (HEK293, His) is 256 a.a., with molecular weight of 35-40 kDa.
Serpin A5 protein is a heparin-dependent serine protease inhibitor that controls proteolytic activity in body fluids. It binds irreversibly to the serine activation site, inactivating serine proteases and regulating intravascular and extravascular proteolysis. Serpin A5 Protein, Mouse (Baculovirus, His) is the recombinant mouse-derived Serpin A5 protein, expressed by Sf9 insect cells , with N-10*His labeled tag. The total length of Serpin A5 Protein, Mouse (Baculovirus, His) is 381 a.a., with molecular weight of ~45.3 kDa.
Serpin G1 Protein, also called C1-inhibitor, regulates complement activation, blood coagulation, fibrinolysis, and kinin generation. It forms inactive complexes with C1r or C1s proteases, controlling C1 complex activation. Serpin G1 efficiently inhibits FXIIa and possibly chymotrypsin and kallikrein, and interacts with MASP1. Its inhibitory effects maintain pathway balance, preventing excessive activation and ensuring proper physiological function. Serpin G1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin G1 protein, expressed by HEK293, with C-6*His labeled tag. The total length of Serpin G1 Protein, Mouse (HEK293, His) is 485 a.a., with molecular weight of 92-95 kDa.
Coagulation factor XI (F11) occupies a central position in the middle phase of the intrinsic pathway of blood coagulation, where it assumes the key role of activating factor IX. This complex process plays a key role in the chain of events that lead to the formation of a blood clot. Coagulation Factor XI/F11 Protein, Human (His) is the recombinant human-derived Coagulation Factor XI/F11 protein, expressed by E. coli , with N-6*His labeled tag. The total length of Coagulation Factor XI/F11 Protein, Human (His) is 369 a.a., with molecular weight of ~45.2 kDa.
Factor IX (F9) is a vitamin K-dependent plasma protein that plays a critical role in the intrinsic pathway of coagulation. Factor IX coordinates the conversion of factor X to its active form in the presence of Ca(2+) ions, phospholipids, and factor VIIIa. Coagulation factor IX/F9 Protein, Human (HEK293, His) is the recombinant human-derived Coagulation factor IX/F9 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Coagulation factor IX/F9 Protein, Human (HEK293, His) is 433 a.a., with molecular weight of 60-90 kDa.
Plasma serine protease inhibitor (SERPINA5) is a glycoproteins that inhibit serine proteases. SERPINA5 is involved in the regulation of intravascular and extravascular proteolytic activities, controls the sperm motility and fertilization and protect components of the genital tract. SERPINA5 also inhibits urinary-type plasminogen activator-dependent tumor cell invasion and metastasis. Serpin A5 Protein, Human (HEK293, His) is the recombinant human-derived Serpin A5 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin A5 Protein, Human (HEK293, His) is 387 a.a., with molecular weight of 44-55 kDa.
CASK protein is a Mg(2+)-independent multidomain scaffold kinase that catalyzes phosphate transfer to proteins, including NRXN1, thereby contributing to synaptic transmembrane protein anchoring and ion channel trafficking. It plays a critical role in neural development, regulation of gene expression through TBR1 interactions, and mediates connections between the extracellular matrix, multiligands, and the actin cytoskeleton. CASK Protein, Human (sf9) is the recombinant human-derived CASK protein, expressed by Sf9 insect cells , with tag free. The total length of CASK Protein, Human (sf9) is 897 a.a., with molecular weight of ~102 kDa.
CASK protein is a Mg(2+)-independent multidomain scaffold kinase that catalyzes phosphate transfer to proteins, including NRXN1, thereby contributing to synaptic transmembrane protein anchoring and ion channel trafficking. It plays a critical role in neural development, regulation of gene expression through TBR1 interactions, and mediates connections between the extracellular matrix, multiligands, and the actin cytoskeleton. CASK Protein, Human (sf9, His-GST) is the recombinant human-derived CASK protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of CASK Protein, Human (sf9, His-GST) is 897 a.a., with molecular weight of ~120 kDa.
PSP94/MSMB protein forms homodimers and interacts with PI16. PSP94/MSMB Protein, Human (His) is the recombinant human-derived PSP94/MSMB protein, expressed by E. coli , with C-His labeled tag. The total length of PSP94/MSMB Protein, Human (His) is 94 a.a., with molecular weight of ~14 kDa.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses. It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups. PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by Sf9 insect cells , with C-Myc, N-10*His labeled tag. The total length of PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is 419 a.a., with molecular weight of 50.7 kDa.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses. It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups. PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by HEK293 , with C-Myc, N-10*His labeled tag. The total length of PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is 419 a.a., with molecular weight of 51.9 kDa.
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine[1]
Linalool-d3 is the deuterium labeled Linalool[1]. Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity[2].Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome[3].
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer .
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
Cholesterol-d is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
Cholesterol-d7 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C3 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6-1 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C5 is the 13C-labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 13C2 is the 13C labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
Cholesterol- 18O is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist .
4-Aminohippuric acid-d4 is the deuterium labeled 4-Aminohippuric acid. 4-Aminohippuric acid is a diagnostic agent, useful in medical tests involving the kidney, used in the measurement of renal plasma flow.
L-Alloisoleucine-d10 is the deuterium labeled L-Alloisoleucine. L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
Hexadecanedioic acid-d28 is the deuterium labeled Hexadecanedioic acid. Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
H-Abu-OH-d3 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
H-Abu-OH-d2 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
H-Abu-OH-d6 is the deuterium labeled H-Abu-OH. H-Abu-OH, one of the three isomers of aminobutyric acid, is elevated in the plasma of children with with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency.
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
Estrone sulfate-d5 (sodium) is the deuterium labeled Estrone sulfate sodium. Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
Estrone sulfate-d4 (sodium) is deuterium labeled Estrone sulfate (sodium). Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer[1][2].
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
VTSEGAGLQLQK- 13C6, 15N2 is the 13C and 15N labeled VTSEGAGLQLQK. VTSEGAGLQLQK is an amino acid sequence in the C-terminal region of recombinant human alpha-acid glucosidase (rhGAA). VTSEGAGLQLQK can be used to bind anti-drug antibodies (ADA) in plasma and quantitatively analyze the therapeutic effect .
VTSEGAGLQLQK- 13C6, 15N2 (TFA) is the 13C- and 15N-labeled VTSEGAGLQLQK. VTSEGAGLQLQK is an amino acid sequence in the C-terminal region of recombinant human alpha-acid glucosidase (rhGAA), which can be used to bind anti-drug antibodies in plasma and quantitatively analyze the therapeutic effect .
Chlorpyrifos-d10 is the deuterium labeled Chlorpyrifos. Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
Losartan carboxylic acid-d4 (hydrochloride) is deuterium labeled Losartan Carboxylic Acid. Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].