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Results for "

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  • Inhibitors & Agonists
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    TargetMol | All_Pathways
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2-Chloroadenosine
T7736146-77-0
2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors( Ki:300, 80, and 1,900 nM, respectively)
  • $43
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L-Arginine hydrochloride
L-arginine monohydrochloride, L-Arginine HCl (L-Arg), (S)-(+)-Arginine hydrochloride
T06701119-34-2
L-Arginine hydrochloride serve as substrates and nitrogen donors for endothelial nitric oxide synthase (eNOS) to produce nitric oxide (NO). They are transported into vascular smooth muscle cells via cationic amino acid transporters, where they are metabolized into NO, polyamines, or L-proline. As effective vasodilators, they are commonly used to induce experimental acute pancreatitis models.
  • $33
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Paclobutrazol
2R,3R-Paclobutrazol, (R,R)-paclobutrazol, (2R,3R)-Paclobutrazol
T3827376738-62-0
Paclobutrazol ((R,R)-paclobutrazol) is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins.1,2It also has antifungal activities.3PBZ, which is transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants.1,4,5PBZ is typically used to support research on the role of gibberellins in plant biology.
  • $34
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L-Arginine
L-Arg, (S)-(+)-Arginine
T3S036474-79-3
L-Arginine (L-Arg) is a substrate for endothelial nitric oxide synthase (eNOS), participating in protein synthesis, polyamine production, and cellular signaling regulation. L-Arginine is transported into vascular smooth muscle cells via the cationic amino acid transporter family and metabolized into nitric oxide, polyamines, or L-proline. L-Arginine is an effective vasodilator and can be used to induce experimental acute pancreatitis.
  • $31
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TargetMol | Citations Cited
D-Ala-Lys-AMCA hydrochloride
T189572703746-41-0
D-Ala-Lys-AMCA hydrochloride, a known substrate of proton-coupled oligopeptide transporter 1 (PEPT1), emits blue fluorescence and may be transported into Caco-2 cells and liver cancer cells.
  • $323
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Anhydroleucovorin
Methyltetrahydrofolic Acid, Methenyltetrahydrofolic Acid, 5,10-Methenyltetrahydrofolic Acid
T2059537444-29-3
Anhydroleucovorin is the predominant, biologically active form of vitamin B9 (folate) that is utilized by the body for a multitude of vital cellular functions, including DNA synthesis, repair, and methylation, as well as the production of key neurotransmitters; Anhydroleucovorin plays an essential metabolic role in the remethylation pathway, converting the amino acid homocysteine to methionine, and serves as the main folate form found in systemic circulation and transported into tissues for physiological use.
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Lysosomal P-gp targeted agent 1
T2061403043797-88-9
Lysosomal P-gp targeted agent 1 (Compound 14) is an antitumor drug that targets lysosomal P-glycoprotein (Pgp). It is selectively transported to lysosomes via overexpressed Pgp, releasing nitric oxide that generates reactive oxygen species (ROS), causing lysosomal membrane permeabilization (LMP) and inducing apoptosis. This compound can overcome resistance mediated by P-glycoprotein, leading to cell cycle arrest while maintaining relatively low toxicity to normal cells. It exhibits antitumor activity by significantly inhibiting tumor growth.
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10-14 weeks
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Albitiazolium bromide
SAR97276
T29834321915-72-4
Albitiazolium bromide is an antimalarial compound that interferes with phospholipid metabolism in Plasmodium parasites, particularly disrupting the biosynthesis of phosphatidylcholine (PC).Albitiazolium bromide gains cellular entry via the new permeability pathways (NPP) of infected erythrocytes before being transported into the parasite by a poly-specific cation carrier, making Albitiazolium bromide an important investigational agent for malaria research.
  • $49
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Levomefolate magnesium
L-Methylfolate magnesium
T327051429498-11-2
Levomefolate magnesium is the magnesium salt of the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma. It is transported across th
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cDPCP
T36745106343-59-3
cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)
  • $296
35 days
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Estradiol 17-(β-D-Glucuronide) (sodium salt hydrate)
T36807
Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)
  • $265
35 days
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N-hexadecanoyl-L-Homoserine lactone
N-palmitoyl-L-Homoserine, N-hexadecanoyl-L-Homoserine lactone, C16-HSL
T3774187206-01-7
Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases.[3] AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family.[4] C16-HSL is one of a number of lipophilic, long acyl side-chain bearing AHLs, including its monounsaturated analog C16:1-(L)-HSL, produced by the LuxI AHL synthase homolog SinI involved in quorum-sensing signaling in S. meliloti, a nitrogen-fixing bacterial symbiont of certain legumes.[5],[6] C16-HSL is the most abundant AHL produced by the proteobacterium R. capsulatus and activates genetic exchange between R. capsulatus cells.[7] N-Hexadecanoyl-L-homoserine lactone and other hydrophobic AHLs tend to localize in relatively lipophilic cellular environments of bacteria and cannot diffuse freely through the cell membrane. The long-chain N-acylhomoserine lactones may be exported from cells by efflux pumps or may be transported between communicating cells by way of extracellular outer membrane vesicles.[8],[9]Reference:[1]. González, J.E., and Keshavan, N.D. Messing with bacterial quorum sensing Microbiol. Mol. Biol. Rev. 70(4), 859-875 (2006).[2]. Gould, T.A., Herman, J., Krank, J., et al. Specificity of acyl-homoserine lactone syntheses examined by mass spectrometry Journal of Bacteriology 188(2), 773-783 (2006).[3]. Cegelski, L., Marshall, G.R., Eldridge, G.R., et al. The biology and future prospects of antivirulence therapies Nature Reviews.Microbiology 6(1), 17-27 (2008).[4]. Penalver, C.G.N., Morin, D., Cantet, F., et al. Methylobacterium extorquens AM1 produces a novel type of acyl-homoserine lactone with a double unsaturated side chain under methylotrophic growth conditions FEBS Letters 580, 561-567 (2006).[5]. Gao, M., Chen, H., Eberhard, A., et al. sinI- and expR-dependent quorum sensing in Sinorhizobium meliloti Journal of Bacteriology 187(23), 7931-7944 (2005).[6]. Teplitski, M., Eberhard, A., Gronquist, M.R., et al. Chemical identification of N-acyl homoserine lactone quorum-sensing signals produced by Sinorhizobium meliloti strains in defined medium Archives of Microbiology 180, 494-497 (2003).[7]. Schaefer, A.L., Taylor, T.A., Beatty, J.T., et al. Long-chain acyl-homoserine lactone quorum-sensing regulation of Rhodobacter capsulatus gene transfer agent production Journal of Bacteriology 184(23), 6515-6521 (2002).[8]. Pearson, J.P., Van Delden, C., and Iglewski, B.H. Active efflux and diffusion are involved in transport of Pseudomonas aeruginosa cell-to-cell signals Journal of Bacteriology 181(4), 1203-1210 (1999).[9]. Mashburn-Warren, L., and Whiteley, M. Special delivery: Vesicle trafficking in prokaryotes Molecular Microbiology 61(4), 839-846 (2006).
  • $95
35 days
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N-octadecanoyl-L-Homoserine lactone
T37743479050-96-9
C18-HSL is one of four lipophilic, long acyl side-chain-bearing N-acylated homoserine lactones (AHLs) produced by the LuxI AHL synthase homolog SinI, involved in quorum sensing signaling in S. meliloti, a nitrogen-fixing bacterial symbiont of the legume [M. sativa]. C18-HSL and other hydrophobic AHLs tend to localize in relatively lipophilic cellular environments and cannot diffuse freely through the cell membrane. These long-chain N-acylhomoserine lactones may be exported from cells by efflux pumps or transported between communicating cells via extracellular outer membrane vesicles. Quorum sensing, a regulatory system used by bacteria to control gene expression in response to cell density, manifests in phenotypes such as biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release, and detection of small diffusible signal molecules called autoinducers, including AHLs, which vary in acyl group length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of carbon-carbon double bonds, conferring signal specificity through LuxR family transcriptional regulators. Regulation of bacterial quorum sensing signaling to inhibit pathogenesis represents a novel approach to antimicrobial therapy in treating infectious diseases.
  • $142
35 days
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Cholesteryl palmitate
T5074601-34-3
Cholesteryl palmitic acid is a cholesteryl ester. A cholesteryl ester is an ester of cholesterol. Fatty acid esters of cholesterol constitute about two-thirds of the cholesterol in the plasma. Cholesterol is a sterol (a combination of steroid and alcohol) and a lipid found in the cell membranes of all body tissues and transported in the blood plasma of all animals. The accumulation of cholesterol esters in the arterial intima (the innermost layer of an artery, in direct contact with the flowing blood) is a characteristic feature of atherosclerosis. Atherosclerosis is a disease affecting arterial blood vessels. It is a chronic inflammatory response in the walls of arteries, in large part to the deposition of lipoproteins (plasma proteins that carry cholesterol and triglycerides).
  • $48
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[Tyr3]Octreotate
T67931302794-43-0
[Tyr3]Octreotate is a long peptide compound containing 8 amino acids and is a functional DOTA chelating agent with covalent bonds. [Tyr3]Octreotate binds to transmembrane receptors of SSR2-active NETs and is actively transported into cells by endocytosis, which may increase the required double-stranded DNA breaks and is a potential drug for tumor treatment.
  • $163
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BGC-638
T69268416852-27-2
BGC-638, an analogue of BGC-945, is a thymidylate synthase inhibitor specifically transported into α-folate receptor (α-FR)–overexpressing tumors.
  • $2,570
10-14 weeks
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Genkwanin
Puddumetin, Apigenin 7-methyl ether, 7-O-Methylapigenin
T6S0095437-64-9
1. Genkwanin (Apigenin 7-methyl ether) exerts its anti-inflammatory effect mainly through the regulation of the miR-11/MKP-1/MAPK pathway. 2. Genkwanin is transported by both passive diffusion and multidrug resistance protein (MDR)-mediated efflux mechanisms.
  • $52
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TargetMol | Citations Cited
Palmitoleoyl-CoA lithium
T88807324518-22-1
Palmitoleoyl-CoA lithium is the lithium salt form of Palmitoleoyl-CoA. It can be activated and transported to mitochondria for metabolism, specifically undergoing β-oxidation. Furthermore, it induces a permeability transition in cardiac mitochondrial membranes, leading to mitochondrial dysfunction. Palmitoleoyl-CoA lithium regulates metabolism through conformational control of the AMPK β1-isoform.
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MHES0488A
T9901A-980
MHES0488A is a selective humanized antibody targeting HER2, with a KD value of 0.8 nM. It constitutes the antibody portion of DHES0815A. Upon cellular internalization, MHES0488A is transported to lysosomes, releasing PBD-monoamide into the nucleus, where it alkylates DNA, inducing DNA damage and apoptosis. It shows potential for research in cancers such as HER2-positive breast cancer and gastric cancer.
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L-Arginine (Standard)
Arginine (Standard)
TMSM-222574-79-3
L-Arginine (Standard) is the reference standard of L-arginine, applicable to quantitative analysis, quality control, biochemical experiments, and related research. L-Arginine (L-Arg) is a substrate for endothelial nitric oxide synthase (eNOS). It is transported into vascular smooth muscle cells via the cationic amino acid transporter family and metabolized to nitric oxide, polyamines, or L-proline. L-Arginine is a potent vasodilator and can be used to induce experimental acute pancreatitis.
  • $36
7-10 days
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Genkwanin (Standard)
TMSM-2961437-64-9
Genkwanin (Standard) is a reference standard for research and analysis in studies involving Genkwanin. 1. Genkwanin (Apigenin 7-methyl ether) exerts its anti-inflammatory effect mainly through the regulation of the miR-11/MKP-1/MAPK pathway. 2. Genkwanin is transported by both passive diffusion and multidrug resistance protein (MDR)-mediated efflux mechanisms.
  • $189
7-10 days
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Anhydroleucovorin (Standard)
TMSM-31727444-29-3
Anhydroleucovorin (Standard) is a reference standard for research and analysis in studies involving Anhydroleucovorin. Anhydroleucovorin is the predominant, biologically active form of vitamin B9 (folate) that is utilized by the body for a multitude of vital cellular functions, including DNA synthesis, repair, and methylation, as well as the production of key neurotransmitters; Anhydroleucovorin plays an essential metabolic role in the remethylation pathway, converting the amino acid homocysteine to methionine, and serves as the main folate form found in systemic circulation and transported into tissues for physiological use.
  • $318
7-10 days
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Docosahexaenoyl-L-carnitine chloride
TN11026
Docosahexaenoyl-L-carnitine chloride is a long-chain acyl-L-carnitine composed of Docosahexaenoic acid and L-carnitine. Under the influence of carnitine palmitoyltransferase I (CPT I) and other enzymes, it is transported to the mitochondria for β-oxidation and breakdown. Docosahexaenoyl-L-carnitine chloride holds potential for research in diseases related to fatty acid metabolism.
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Palmitoyl coenzyme A
Palmitoyl coenzyme A, Palmitoyl CoA
TXB-001051763-10-6
Palmitoyl coenzyme A is an acyl-CoA thioester that is transported into the mitochondrial matrix via the carnitine shuttle system, where it participates in β-oxidation. Additionally, Palmitoyl coenzyme A serves as a substrate in sphinganine biosynthesis.
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