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GlyR antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (4) Autophagy (4) Endogenous Metabolite (1) GABA Receptor (2) iGluR (1) Isotope-Labeled Compounds (2) Microtubule/Tubulin (4) NOD-like Receptor (NLR) (4)
By Research Areas:	Cancer (4) Metabolic Disease (1) Neurological Disease (3)

8

Inhibitors & Agonists

5

Natural
Products

2

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

Licostinel ACEA-1021	iGluR	Neurological Disease
Licostinel (ACEA-1021) is a glycine receptor antagonist (IC₅₀: 59 nM). Licostinel has neuroprotective activity .

Picrotin	GABA Receptor	Neurological Disease
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for *GlyRs* with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

Colchicine-d6	Isotope-Labeled Compounds Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis	Cancer
Colchicine-d₆ is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].

Guanidinoethyl sulfonate Taurocyamine	Endogenous Metabolite	Metabolic Disease
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC₅₀=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABA_A receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

Colchicine 35+ Cited Publications	Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis	Cancer
Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC₅₀ of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .

Colchicine-d3	Isotope-Labeled Compounds Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis	Cancer
Colchicine-d₃ is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].

Picrotin (Standard)	GABA Receptor	Neurological Disease
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

Colchicine (Standard)	Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis	Cancer
Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .

Cat. No.	Product Name	Category	Target	Chemical Structure

Picrotin	Structural Classification other families Iridoids Terpenoids Source classification Plants	GABA Receptor
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for *GlyRs* with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

Guanidinoethyl sulfonate Taurocyamine	Structural Classification Natural Products Other disease Classification of Application Fields Disease markers Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC₅₀=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABA_A receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .

Colchicine 35+ Cited Publications	Structural Classification Natural Products other families Classification of Application Fields Source classification Plants Disease Research Fields Cancer	Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis
Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC₅₀ of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .

Picrotin (Standard)	Structural Classification other families Iridoids Terpenoids Source classification Plants	GABA Receptor
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

Colchicine (Standard)	Structural Classification Natural Products other families Source classification Plants	Microtubule/Tubulin NOD-like Receptor (NLR) Autophagy Apoptosis
Colchicine (Standard) is the analytical standard of Colchicine. This product is intended for research and analytical applications. Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research .

Cat. No.	Product Name	Chemical Structure

Colchicine-d6
Colchicine-d₆ is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].

Colchicine-d3
Colchicine-d₃ is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].

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