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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC48212 D-(-)-3-Phosphoglyceric acid disodium
D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalysed process of glycolysis. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase.
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DC48211 ARG1-IN-1
ARG1-IN-1 is a human arginase 1 inhibitor with an IC50 of 29 nM.
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DC48210 Alacepril
Alacepril (Cetapril) is an orally active angiotensin converting enzyme (ACE) inhibitor with long lasting antihypertensive effect.
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DC48209 Fasidotril
Fasidotril is a dual inhibitor of neprilysin and angiotensin-converting enzyme (ACE) for the potential treatment of hypertension and congestive heart failure (CHF).
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DC48208 Motugivatrep
Motugivatrep is the potent antagonist of transient receptor potential type 1 (TRPV1). Motugivatrep has a wide range of usefulness in treating drugs, urine tabletops, and respiratory diseases (extracted from patent WO2007010383A1).
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DC48207 TRPV4 antagonist 3
TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).
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DC48206 TRPA1-IN-1
TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.
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DC48205 Oleoyl serotonin
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1.
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DC48203 S-Bioallethrin
S-Bioallethrin is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels.
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DC48202 Bliretrigine
Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain.
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DC48201 SGLT1/2-IN-2
SGLT1/2-IN-2 demonstrates potent dual inhibitory activities (IC50 = 96 nM for SGLT1 and IC50 = 1.3 nM for SGLT2).
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DC48200 Cibenzoline
Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy.
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DC48199 Isoallolithocholic acid
Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes.
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DC48198 S-(+)-Mecamylamine hydrochloride
S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.
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DC48197 UBP301
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine.
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DC48196 Onfasprodil
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A).
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DC48195 GluN2B receptor modulator-1
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
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DC48194 Aptiganel hydrochloride
Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
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DC48193 Arbaclofen placarbil
Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
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DC48192 Adipiplon
Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.
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DC48189 Xestospongin C
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells.
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DC48188 HSK16149
HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit.
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DC48187 PIM-IN-1
PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC50 = 61 nM; pS6, EC50 = 71 nM).
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DC48186 Povorcitinib
Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1).
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DC48185 JAK1/TYK2-IN-1
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM respectively).
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DC48184 TLR7/8 agonist 4 TFA
TLR7/8 agonist 4 TFA (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity.
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DC48183 Ruzotolimod
Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1).
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DC48182 Poly(I:C)
Poly(I:C) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Poly(I:C) present in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA.
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DC48181 Polvitolimod
Polvitolimod is a TLR7 agonist for treatment of cancer and infectious disease.
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DC48180 GSK1795091
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines.
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