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Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI50 value of 6.96 and Ki value of 2.4 nM for humanplasma cholinesterase (ChE) .
Plasminogen, Humanplasma 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 .
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 .
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 .
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 .
Teneligliptin hydrobromide hydrate is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits humanplasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
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 .
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 .
Teneligliptin (MP-513) hydrobromide is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits humanplasma, 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 humanplasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
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 .
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits humanplasma, 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 humanplasma and has significant fibrinolytic activity by activating the fibrinolytic system.
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].
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 .
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 .
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in humanplasma (IC50 36 nM) in vitro.
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 .
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of humanplasma (albeit at low levels).
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 humanplasma samples after oral administration of Ezetimibe (HY-17376) .
Feniralstat (compound 30), a pyrazole derivative, is a potent kallikrein inhibitor with an IC50 of 6.7 nM for Humanplasma kallikrein (pKal). Feniralstat has no inhibition on Human KLKl, Human FXIa, Human Factor Xlla (all IC50>40 μM).
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole humanplasma, having a CETP concentration of 37 nM .
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 humanplasma CETP, 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.
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 .
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 .
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 .
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 humanplasma 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.
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 .
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 humanplasma (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 .
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and humanplasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
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 humanplasma.
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 .
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 humanplasma. 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 .
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 .
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 .
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, humanplasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research .
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.
Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits humanreninand humanplasmarenin 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 .
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 .
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 .
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) .
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 .
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 humanplasma clot lysis assay .
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 humanplasma, respectively. Vidupiprant has the potential for asthma treatment .
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 .
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in humanplasma. 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 humanplasma. 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].
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 .
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 .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in humanplasma 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.
TZ4M is a 2,4-thiazolidinedione (TZD)-based anti-ADV agent with neuroprotective effects. TZ4M exhibits AChE inhibition in humanplasma. TZ4M improves memory and cognitive impairment in adult rats in a scopolamine (HY-N0296)-induced Alzheimer-type model .
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.
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 .
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 .
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 .
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 humanplasma and the best pharmacological profile .
(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 .
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 humanplasma 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) .
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 .
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 .
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 .
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 humanplasma 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 humanplasma 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 humanplasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally .
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.)
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 .
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 humanplasma 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.
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 .
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 .
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].
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.
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 .
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 .
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 .
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 humanplasma 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.
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 .
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 .
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 .
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 .
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 .
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 .
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.
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) .
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 .
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.)
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 .
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 .
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 .
3-Methylsalicylic acid is a salicylic acid derivative that acts on humanplasma and has significant fibrinolytic activity by activating the fibrinolytic system.
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 .
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 .
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of humanplasma (albeit at low levels).
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 .
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 humanplasma.
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 .
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in humanplasma 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.
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 .
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) 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 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.
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.
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.
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.
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.
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.
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.
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.
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].
O-Desmethyl gefitinib-d8 is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in humanplasma. 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].
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 .
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits humanplasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
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 humanplasma (albeit at low levels).
O-Desmethyl gefitinib-d6 is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in humanplasma. 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].
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.
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 humanplasma 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.
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].
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