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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC41144 Remdesivir nucleoside monophosphate
Remdesivir nucleoside monophosphate is a metabolite of Remdesivir. Remdesivir is a nucleoside analogue with effective antiviral activity against SARS-CoV and MERS-CoV.
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DC41137 1-Aminocyclobutanecarboxylic acid
1-Aminocyclobutanecarboxylic acid is a NMDA receptor partial agonist acting at the glycine site, NR1.
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DC41136 PYBG
PYBG acts as a versatile precursor to be facilely conjugated with various fluorescent dyes through ‘Click chemistry’ and Sonogashira coupling reactions.
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DC41135 4-Ethynyl-L-phenylalanine hydrochloride
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin.
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DC41133 Org-12962 hydrochloride
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C?receptor agonist and exhibits pEC50?values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A?and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.
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DC41132 Contezolid acefosamil
Contezolid acefosamil (MRX-4) is the orally active prodrug of the active antimicrobial metabolite Contezolid (MRX-I), an oxazolidinone which shows potent in vitro activity against various multidrug-resistant Gram-positive bacteria, including MRSA
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DC41131 Brilacidin tetrahydrochloride
Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is an anti-infective antimicrobial with MIC90s of 1 and 8 μg/mL for Gram-positive bacteria Streptococcus pneumonia and Streptococcus viridans, and MIC90 of 8 and 4 μg/mL for Gram-negative bacteria Haemophilus influenza and Pseudomonas aeruginosa. Brilacidin tetrahydrochloride is a defensin mimetic antibiotic compound.
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DC41130 (Z)-4EGI-1
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
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DC41128 Sitamaquine tosylate
Sitamaquine (WR 6026) tosylate, an orally active 8-aminoquinoline analog, is an antileishmanial agent. Sitamaquine is a lipophilic weak base that rapidly accumulates in acidic compartments of Leishmania spp., mainly in acidocalcisomes.
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DC41127 EGFR-IN-1 TFA
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
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DC41126 Nikkomycin Z
Nikkomycin Z, a nucleoside-peptide, is a selective competitive chitin synthesis inhibitor. Nikkomycin Z has antifungal effects and acts as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine.
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DC41125 Isamoltane hemifumarate
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
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DC41124 AVE3085
AVE3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.
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DC41123 GYKI-47261 dihydrochloride
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1.
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DC41122 cis-ACPD
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
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DC41121 SSR180711 hydrochloride
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
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DC41120 AE-3763
AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.
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DC41119 Sulprostone
Sulprostone (SHB 286) is a potent and selective EP3 receptor agonist. Sulprostone (SHB 286) is a prostaglandin E2 (PGE2) analogue and has antiulcer and nonsteroidal abortifacient effects. Sulprostone has potential for the research of pregnancy termination and hemorrhages during delivery.
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DC41118 EMD 56551
EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.
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DC41117 KB-5492 anhydrous
KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.
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DC41116 Merbarone
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent.
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DC41115 MCT1-IN-2
MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity.
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DC41114 AMI-1 free acid
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
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DC41113 NCT-501 hydrochloride
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
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DC41112 NSC-87877 disodium
NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
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DC41111 CP-465022 hydrochloride
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50?of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
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DC41110 VEGFR-2-IN-5 hydrochloride
VEGFR-2-IN-5 hydrochloride is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 69.
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DC41109 SB-215505
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
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DC41108 2,4-D sodium salt
2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D sodium salt acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D sodium salt inhibits DNA and protein synthesis and thereby prevents normal plant growth and development.
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DC41107 3-Indoleacetic acid-D5
3-Indoleacetic acid-D5 (Indole-3-acetic acid-D5) is the deuterium labeled 3-Indoleacetic acid. 3-Indoleacetic acid-D5 can be used as internal standard for assay of IAA releases by alkaline hydrolysis of ester and amide conjugates.
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