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  • Inhibitors & Agonists
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    TargetMol | Inhibitors_Agonists
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Iptacopan hydrochloride
LNP023 hydrochloride, Iptacopan HCl
T91891646321-63-2In house
Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.
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TargetMol | Inhibitor Hot
(Rel)-Factor B-IN-5
T626892760789-22-6In house
(Rel)-Factor B-IN-5 is a complement factor B inhibitor that can be used to study diseases associated with activation of the alternative complement pathway.
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10-14 weeks
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Fosphenytoin
T6135493390-81-9In house
Fosphenytoin is a phosphate prodrug that can be used as an alternative to intravenous phenytoin for the acute intervention of seizures.Fosphenytoin is hydrolyzed to anticonvulsant phenytoin when administered parenterally.Fosphenytoin can be used in a variety of delivery modes such as intravenous and intraperitoneal.Fosphenytoin can be used in a variety of delivery modes such as intravenous and intraperitoneal.
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6-8 weeks
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3-Hydroxykynurenamine
T6818299362-47-7In house
3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1 NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.
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3-6 months
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AZD-4877
AZD4877
T9682758722-49-5In house
AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).
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Chlorophyllin sodium copper salt
Chlorophyllin copper sodium complex, Chlorophyllin coppered trisodium salt
T125411006-34-1
Chlorophyllin sodium copper salt (Chlorophyllin coppered trisodium salt) is a semi-synthetic mixture of water-soluble sodium copper salts derived from chlorophyll, primarily used as a food additive and alternative medicine.
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TargetMol | Citations Cited
Ethyl gallate
Nipagallin A, Phyllemblin, gallic acid ethyl ester
T3729831-61-8
Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9 MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2 Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.
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TargetMol | Citations Cited
MONOCAPRYLIN
Sefsol 318, Glyceryl monocaprylate
T950826402-26-6
Monocaprylin (Sefsol 318) is a monoglyceride of caprylic acid with an excellent antibacterial activity. Monocaprylin inhibits a variety of foodborne pathogenic and spoilage microorganisms and has the potential for an alternative food preservative research.
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Levomefolate calcium
T7593151533-22-1
Levomefolate calcium, an artificial form of folate, is a coenzymated form of folic acid that offers a more bioavailable alternative in dietary supplements.
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L-Ascorbic acid sodium salt
(+)-Sodium L-ascorbate, Vitamin C sodium salt, Sodium ascorbate, L-Ascorbic acid sodium, Sodium L-ascorbate
T6674134-03-2
L-Ascorbic acid sodium salt (Vitamin C sodium salt) is a more bioavailable form of vitamin C that is an alternative to taking ascorbic acid as a supplement.
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L-Alanyl-L-glutamine
Ala-Gln
T559339537-23-0
L-Alanyl-L-glutamine (Ala-Gln), a dipeptide composed of alanine and Gln, is an alternative supplement to L-glutamine in the production of biopharmaceuticals with better solubility and stability than glutamine (Gln).
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Abeprazan
DWP14012
T10221L1902954-60-2In house
Abeprazan (DWP14012) is a potassium-competitive acid blocker developed as a potential alternative to proton pump inhibitors for treating acid-related diseases. It inhibits H+, K+-ATPase through reversible potassium-competitive ionic binding, without requiring acid activation [1].
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6-8 weeks
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GSK591
GSK3203591, EPZ015866
T68531616391-87-7
GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
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TargetMol | Citations Cited
Compstatin
TP1304206645-99-0
Compstatin is a cyclic peptide consisting of 13 amino acid residues and is a potent inhibitor of complement system C3. Compstatin is species-specific and has inhibitory effects only on the complement system of primates. Studies have shown that it can bind to baboon C3 and is resistant to proteolytic cleavage in baboon blood. Its IC50 values for the classical pathway and alternative pathway are 63 μM and 12 μM, respectively.
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TargetMol | Citations Cited
NHC-diphosphate triammonium
T36881
NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2]. In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours[1].NHC-triphosphate triammonium (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions[1].Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS/MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate triammonium remains the most abundant metabolite[2].NHC-triphosphate triammonium (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator. It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation. [1]. Stuyver LJ,et al. Ribonucleoside analogue that blocks replication of bovine viral diarrhea and hepatitis C viruses in culture.Antimicrob Agents Chemother. 2003 Jan;47(1):244-54. [2]. Maryam Ehteshami, et al. Characterization of β-d- N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus.
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Antioxidant peptide A
TP1869
Antioxidant peptide A is a short peptide containing alternating aromatic or sulfur-containing amino acids (alternative aromatic or sulfur-containing amino acid).
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CELT-327
T83958
CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptors in a dose-dependent manner, demonstrating rapid, uniform spread and integration of fluorescence within cell monolayers. In live HCT116 spheroids, it achieves consistent staining throughout, penetrating even the deepest layers. As a fluorescent adenosine receptor probe, CELT-327 is ideal for applications in fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays, serving as an effective alternative to GPCR radiolabeling ligands. Its excitation and emission peaks are at 589 nm and 616 nm, respectively, making it suitable for TR-FRET assays as an acceptor dye, particularly in combination with the CoraFlor1 TR-FRET donor.
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AL 8810 ethyl amide
T38114
AL 8810 is an 11β-fluoro analog of prostaglandin F2α (PGF2α) which acts as a potent and selective antagonist at the FP receptor. AL 8810 ethyl amide is an analog of AL 8810 in which the C-1 carboxyl group has been modified to an N-ethyl amide. This modification is analogous to the PG N-ethyl amides, as typified by Bimatoprost, that have been introduced as alternative PG ocular hypotensive prodrugs. In contrast to AL 8810 which contracted the cat iris, AL 8810 ethyl amide showed no contraction activity at concentrations up to 10-4 M and did not antagonize the activity of PGF2α-ethanolamide in this system.
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DEPMPO-biotin
T36027936224-52-1
DEPMPO is a nitrone that is used to spin trap reactive O-, N-, S-, and C-centered radicals and allow their characterization when used in association with electron spin resonance. It is noted for the stability of adducts formed. DEPMPO can be used in vitro or in vivo, as it crosses lipid bilayer membranes and is a good trapping agent in biological systems. DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective means for monitoring biodistribution in cells, tissues, and organs when used with an avidin-conjugated reporter. Importantly, DEPMPO-biotin binds free radicals, such as S-nitroso groups, on proteins, producing adducts that can be analyzed via the biotin tag. This direct labeling of S-nitrosothiols (SNO) thus serves as an effective alternative to the more cumbersome biotin-switch method for monitoring SNO formation.
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Fluorescein-NAD+
T36304
Fluoroscein NAD+ is a substrate for ADP-ribosylation, providing a convenient non-isotopic alternative to radiolabelled NAD for use in PARP assays. Allows direct measurement of NAD-dependent enzymes, such as PARP, by fluorescence microscopy. This product is a replacement for R&D Systems product 4673-500-01 81 μg is supplied as 250 μl of a 0.25 mM solution in water.
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Ascofuranone
T6931338462-04-3
Ascofuranone is an inhibitor of the ubiquinol oxidase activity of Trypanosoma brucei mitochondrial alternative oxidase (TAO), as well as an inhibitor of HsDHODH.
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10-14 weeks
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NHC-triphosphate tetrasodium
T74070
NHC-triphosphate tetrasodium, the active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) in its triphosphate form, functions as a weak alternative substrate for viral polymerase, allowing its incorporation into HCV replicon RNA.
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Eprociclovir potassium
T70027219657-37-1
Eprociclovir potassium is a new acyclovir analogue and a potent inhibitor of EHV1 replication and may have potential for the treatment and or prophylaxis of infections with this virus. Eprociclovir possess potent anti-herpetic activity against most human herpesviruses. A-5021 proved to be about 15-fold more potent than acyclovir in inhibiting viral replication. Eprociclovir inhibits murine herpetic keratitis. A-5021 eyedrops, which are easily applied onto the affected cornea, ameliorated clinical scores and suppressed virus growth. Eprociclovir is a promising alternative treatment of herpetic keratitis.
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1-2 weeks
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2,4-Decadienal
TYD-007152363-88-4
2,4-Decadienal is a toxic aldehyde produced by the oxidation of linoleic acid-rich oils. It serves as an alternative oxidation indicator for oils rich in linoleic acid.
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