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transmembrane site

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bacterial (1) Calcium Channel (1) Caspase (1) GCGR (3) Hedgehog (1) mGluR (2) nAChR (2) Parasite (1) Ser/Thr Protease (1) Smo (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Infection (2) Metabolic Disease (3) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Targets Recommended: CFTR Enteropeptidase BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-110087

4BP-TQS	nAChR	Neurological Disease
4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .

HY-141839

GLP-1R modulator C16	GCGR	Metabolic Disease
GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 8.43 ± 3.82 μM).

HY-141840

GLP-1R modulator C5	GCGR	Metabolic Disease
GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 1.59 ± 0.53 μM).

HY-141842

GLP-1R modulator L7-028	GCGR	Metabolic Disease
GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC₅₀ 11.01 ± 2.73 μM).

HY-108507

MRT-10	Smo	Cancer
MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC₅₀ of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .

HY-103565

AMN082	mGluR	Neurological Disease
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .

HY-103565A

AMN082 free base	mGluR	Neurological Disease
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .

HY-117903A

MRT-92	Smo Hedgehog	Cancer
MRT-92 is a Smoothened (Smo) antagonist (K_i=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC₅₀=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .

HY-117005

C450-0730	Bacterial	Infection
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitory activity of C450-0730 against LuxN ^I209F was not significant .

HY-111161

GSK575594A	nAChR Parasite	Infection
GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (E_max increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies .

HY-137038

N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride TLCK hydrochloride	Caspase Ser/Thr Protease	Cancer
N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serine protease, which inhibits trypsin and trypsin-like protease by alkylating histidine residues in their active site. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC₅₀s of 12.0, 54.5 and 19.3 μM, respectively. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembrane potential during apoptosis .

HY-101390A

(-)-Niguldipine hydrochloride (R)-Niguldipine hydrochloride	Calcium Channel	Cardiovascular Disease
(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID₅₀ of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (K_i of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED₃₀ of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .

Cat. No.	Product Name

HY-L062

Neurotransmitter Receptor Compound Library	1,915 compounds
Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding. In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy. MCE designs a unique collection of 1,915 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

Neurotransmitter Receptor Compound Library

1,915 compounds

Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.

In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.

MCE designs a unique collection of 1,915 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

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