Search Result

Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

brain membranes

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (1) Adrenergic Receptor (4) Akt (1) Angiotensin Receptor (1) Autophagy (3) Bacterial (4) Biochemical Assay Reagents (2) Cannabinoid Receptor (3) Deubiquitinase (1) Drug Metabolite (1) EAAT (1) Endogenous Metabolite (3) FAAH (1) Ferroptosis (1) Fungal (1) GABA Receptor (4) GlyT (1) Histone Methyltransferase (1) iGluR (4) Isotope-Labeled Compounds (2) Ligands for Target Protein for PROTAC (1) mAChR (1) MAGL (3) Mitophagy (2) nAChR (1) Neurokinin Receptor (3) Opioid Receptor (3) p38 MAPK (1) Potassium Channel (2) Proteasome (1) Reactive Oxygen Species (1) Sigma Receptor (2) TGF-β Receptor (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (5) Endocrinology (5) Infection (4) Inflammation/Immunology (9) Metabolic Disease (7) Neurological Disease (35)

By Targets:

5-HT Receptor (3)

Adenosine Receptor (1)

Adrenergic Receptor (4)

Akt (1)

Angiotensin Receptor (1)

Autophagy (3)

Bacterial (4)

Biochemical Assay Reagents (2)

Cannabinoid Receptor (3)

Deubiquitinase (1)

Drug Metabolite (1)

EAAT (1)

Endogenous Metabolite (3)

FAAH (1)

Ferroptosis (1)

Fungal (1)

GABA Receptor (4)

GlyT (1)

Histone Methyltransferase (1)

iGluR (4)

Isotope-Labeled Compounds (2)

Ligands for Target Protein for PROTAC (1)

mAChR (1)

MAGL (3)

Mitophagy (2)

nAChR (1)

Neurokinin Receptor (3)

Opioid Receptor (3)

p38 MAPK (1)

Potassium Channel (2)

Proteasome (1)

Reactive Oxygen Species (1)

Sigma Receptor (2)

TGF-β Receptor (1)

By Research Areas:

Cancer (11)

Cardiovascular Disease (5)

Endocrinology (5)

Infection (4)

Inflammation/Immunology (9)

Metabolic Disease (7)

Neurological Disease (35)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18698

L-701324	iGluR	Neurological Disease
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC₅₀=2 nM). L-701324 has antidepressant activity .

HY-15084

Dizocilpine maleate Maximum Cited Publications 25 Publications Verification MK-801 maleate	iGluR	Neurological Disease
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with K_d of 37.2 nM in rat brain membranes.

HY-110256

N-Acetylcysteine amide 5+ Cited Publications	Reactive Oxygen Species	Neurological Disease Inflammation/Immunology
N-Acetylcysteine amide is a cell membranes and blood brain barrier permeant thiol antioxidant and neuroprotective agent, reduces ROS production.

HY-148246

MU1700	TGF-β Receptor	Cancer
MU1700 is an orally active and potent ALK1/2 inhibitor with IC₅₀s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability .

HY-P3883

[DAla4] Substance P (4-11)	Neurokinin Receptor	Neurological Disease
[DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of ¹²⁵I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC₅₀ of 0.5 μM) and ¹²⁵I-Bolton Hunter-conjugated Substance P (IC₅₀ of 0.15 μM) to rat brain cortex membranes .

HY-13510

Cutamesine dihydrochloride 1 Publications Verification SA4503 dihydrochloride; AGY94806 dihydrochloride	Sigma Receptor	Neurological Disease
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes.

HY-119696S

MTIC-d3	Isotope-Labeled Compounds Drug Metabolite	Neurological Disease Cancer
MTIC-d₃ is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].

HY-100821

2,4-Dihydroxyphenylacetylasparagine
2,4-Dihydroxyphenylacetylasparagine is a potent and selective antagonist of glutamate. 2,4-Dihydroxyphenylacetylasparagine inhibits glutamate binding to rat brain synaptic membranes .

HY-12332

JW 642 1 Publications Verification	MAGL	Neurological Disease
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.

HY-W017540

Cyclocreatine 1 Publications Verification	Others	Cardiovascular Disease
Cyclocreatine is a Creatine analogue and acts as a potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine crosses membranes, enters the brain, and can be phosphorylated and dephosphorylated by creatine kinases .

HY-14136

Rimonabant 5 Publications Verification SR141716	Cannabinoid Receptor Bacterial	Infection Metabolic Disease Cancer
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a K_i of 1.8 nM. Rimonabant (SR141716) also inhibits *Mycobacterial membrane* protein Large 3 (MMPL3)**.

HY-160791

Claramine	Others	Infection Cancer
Claramine is a steroid polyamine with blood-brain barrier permeability. Claramine can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins .

HY-10712

Org-24598	GlyT	Neurological Disease
Org-24598 is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 can inhibit the specific binding of [ ³H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM .

HY-100937

DPCPX 4 Publications Verification PD 116948	Adenosine Receptor	Cardiovascular Disease
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a K_i of 0.46 nM in ³H-CHA binding to A1 receptors in rat whole brain membranes .

HY-102064

SR 57227A 1 Publications Verification	5-HT Receptor	Neurological Disease
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC₅₀) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .

HY-15249

JZL 184 2 Publications Verification	MAGL	Neurological Disease
JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC₅₀ of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH .

HY-A0160

Indalpine LM 5008
Indalpine (LM 5008) is a potent and selective 5-HT uptake blocker. Indalpine is potent in displacing ³H-5-HT bound to brain membranes with the IC₅₀ of 36 μM . Indalpine, two antidepressant agent .

HY-18236

MDL-28170 5+ Cited Publications Calpain Inhibitor III	Proteasome	Neurological Disease Inflammation/Immunology
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration . MDL-28170 also block γ-secretase .

HY-59201A

A-582941 dihydrochloride	nAChR 5-HT Receptor	Neurological Disease
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with K_is of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT₃ receptor with a K_i of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .

HY-15084B

Dizocilpine MK-801	iGluR	Neurological Disease
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a K_d of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca ²⁺ flux .

HY-118140

ZCZ011	Cannabinoid Receptor	Neurological Disease Inflammation/Immunology
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .

HY-14136S

Rimonabant-d10 SR141716-d₁₀	Isotope-Labeled Compounds Cannabinoid Receptor Bacterial	Infection Metabolic Disease Cancer
Rimonabant-d₁₀ is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-150407

TSPO ligand-1	Ligands for Target Protein for PROTAC Autophagy	Others Neurological Disease Cancer
TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .

HY-10864

URB-597 4 Publications Verification KDS-4103	FAAH Autophagy Mitophagy	Neurological Disease
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC₅₀s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .

HY-U00322

5-HT3 antagonist 3	5-HT Receptor	Neurological Disease
5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with K_i of 0.25 nM .

HY-119033

MGL-IN-1	MAGL	Inflammation/Immunology
MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant .

HY-108483

RP 67580	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a K_i value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .

HY-131688

2-Chlorohexadecanoic acid	Others	Inflammation/Immunology
2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .

HY-107855S

DL-Mevalonolactone-d7 (±)-Mevalonolactone-d₇; Mevalolactone-d₇	Endogenous Metabolite	Metabolic Disease
DL-Mevalonolactone-d₇ is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].

HY-111544

EML741	Histone Methyltransferase	Cancer
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC₅₀ of 23 nM, K_d of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC₅₀, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .

HY-P3138

(Sar1)-Angiotensin II	Angiotensin Receptor	Cardiovascular Disease
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a K_d of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes .

HY-107855S1

DL-Mevalonolactone-d3 (±)-Mevalonolactone-d₃; Mevalolactone-d₃	Endogenous Metabolite	Metabolic Disease
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].

HY-160019

MTX115325	Deubiquitinase Mitophagy	Neurological Disease
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC₅₀=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC₅₀=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .

HY-W686216

VK-28	Ferroptosis	Neurological Disease
VK-28, a brain-permeable iron chelator, inhibits both basal and Fe/ascorbate-induced mitochondrial membrane lipid peroxidation, with an IC₅₀ of 12.7 μM. VK-28 exhibits significant neuroprotective effects on ICV-6-OHDA. VK-28 can be used for the research of Parkinson’s disease and other neurodegenerative diseases .

HY-19578B

Isamoltane hemifumarate
Isamoltane hemifumarate is a selective antagonist of 5-HT_1B receptor, with an IC₅₀ of 39 nM for inhibits the binding of [ ¹²⁵I]ICYP to 5-HT_1B 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 .

HY-120645

BMS-986122	Opioid Receptor	Neurological Disease
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ ³⁵S]GTPγS binding in mouse brain membranes .

HY-E70007

Catechol O-methyltransferase, porcine liver COMT	Endogenous Metabolite	Neurological Disease
Catechol O-methyltransferase, porcine liver (COMT), the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain .

HY-10061

Lesogaberan AZD-3355	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-10061B

Lesogaberan hydrochloride AZD-3355 hydrochloride	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-144632

Antifungal agent 22	Fungal	Infection
Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC₅₀ of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .

HY-B1102

Evans Blue 5+ Cited Publications Direct Blue 53; T-1824; C.I. 23860	EAAT iGluR	Neurological Disease
Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .

HY-W018643

Ferulic acid methyl ester Methyl ferulate	p38 MAPK Autophagy	Neurological Disease Inflammation/Immunology Cancer
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties . Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders . Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages .

HY-P1318

Ac-RYYRIK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P1318A

Ac-RYYRIK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-10061A

Lesogaberan napadisylate AZD-3355 napadisylate	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan napadisylate for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-115340

Decanoic acid sodium	Biochemical Assay Reagents	Others
Decanoic acid sodium, also known as Decanoic acid sodium, is a salt of the fatty acid capric acid. It is easily soluble in water and has a slightly soapy smell. Decanoic acid sodium acts as a penetration enhancer, which means it increases the absorption and bioavailability of drugs across biological membranes, including the intestinal epithelium and the blood-brain barrier. This property makes it useful in pharmaceutical formulations to improve drug delivery and effectiveness. Furthermore, Decanoic acid sodium has potential applications in food preservatives and cosmetics due to its antibacterial properties.

HY-B0573

Propranolol hydrochloride 15+ Cited Publications	Adrenergic Receptor Bacterial	Neurological Disease Endocrinology Cancer
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol 15+ Cited Publications	Adrenergic Receptor Bacterial	Cardiovascular Disease Neurological Disease Endocrinology Cancer
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-124424

VU0071063	Potassium Channel	Others Neurological Disease
VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC₅₀=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships .

HY-B1055

Pentoxyverine citrate Carbetapentane citrate	Sigma Receptor mAChR	Neurological Disease Inflammation/Immunology
Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .

Cat. No.	Product Name

HY-L043

Lipid Compound Library

1352 compounds

Lipids are a diverse and ubiquitous group of compounds which have many key biological functions, such as acting as structural components of cell membranes, serving as energy storage sources and participating in signaling pathways. Several studies suggest that bioactive lipids have effects on the treatment of some mental illnesses and metabolic syndrome. For example, DHA and EPA are important for monoaminergic neurotransmission, brain development and synaptic functioning, and are also correlated with a reduced risk of cancer and cardiovascular disease in clinical and animal studies.

MCE supplies a unique collection of 1352 lipid and lipid derivative related compounds including triglycerides, phospholipids, sphingolipids, steroids and their structural analogues or derivatives. MCE lipid compound library can be used for research in bioactive lipids, and high throughput screening (HTS) and high content screening (HCS).

HY-L165

Dopamine Receptor Compound Library

195 compounds

Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life.

MCE designs a unique collection of 195 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Cat. No.	Product Name	Type

HY-B1102

Evans Blue

5+ Cited Publications

Direct Blue 53; T-1824; C.I. 23860

Cell Assay Reagents

Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .

HY-115340

Decanoic acid sodium

Biochemical Assay Reagents

Decanoic acid sodium, also known as Decanoic acid sodium, is a salt of the fatty acid capric acid. It is easily soluble in water and has a slightly soapy smell. Decanoic acid sodium acts as a penetration enhancer, which means it increases the absorption and bioavailability of drugs across biological membranes, including the intestinal epithelium and the blood-brain barrier. This property makes it useful in pharmaceutical formulations to improve drug delivery and effectiveness. Furthermore, Decanoic acid sodium has potential applications in food preservatives and cosmetics due to its antibacterial properties.

HY-125139

omega-3 Arachidonic acid ethyl ester

ω-3 Arachidonic acid ethyl ester; (all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester

Biochemical Assay Reagents

omega-3 Arachidonic Acid ethyl ester is a rare polyunsaturated fatty acid found in very small amounts in dietary sources. Omega-3 fatty acids are known to be essential for the growth and development of infants, and they protect against heart disease, blood clots, high blood pressure, and inflammatory and autoimmune diseases. In human platelet membranes, omega-3 arachidonic acid inhibits arachidonyl-CoA synthetase with a Ki of 14 μM. It also inhibits arachidonoyl-CoA synthetase in calf brain extract with an IC50 of approximately 5 μM. Omega-3 ethyl arachidonate is the more lipophilic form of the free acid.

Cat. No.	Product Name	Target	Research Area

HY-P3138

(Sar1)-Angiotensin II	Angiotensin Receptor	Cardiovascular Disease
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a K_d of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes .

HY-P3883

[DAla4] Substance P (4-11)	Neurokinin Receptor	Neurological Disease
[DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of ¹²⁵I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC₅₀ of 0.5 μM) and ¹²⁵I-Bolton Hunter-conjugated Substance P (IC₅₀ of 0.15 μM) to rat brain cortex membranes .

HY-P10153

gH625	Peptides	Others
gH625 is a cell-penetrating viral peptide which is a part of glycoprotein H of Herpes simplex virus type I. gH625 is able to cross the cell membrane and to transport many conjugated cargoes into the cytosol. gH625 is permeable to the blood-brain barrier (BBB) and can enter the rat brain in vivo without toxic effects. gH625 can be used for siRNA delivery research .

HY-P1318

Ac-RYYRIK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P1318A

Ac-RYYRIK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P3071

ShK toxin	Potassium Channel	Inflammation/Immunology
ShK toxin blocks voltage-dependent potassium channel (K_v1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-E70007

Catechol O-methyltransferase, porcine liver COMT	Structural Classification Natural Products Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Catechol O-methyltransferase, porcine liver (COMT), the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain .

HY-W018643

Ferulic acid methyl ester Methyl ferulate	Monophenols Classification of Application Fields Neurological Disease Simple Phenylpropanols Stemonaceae Source classification Phenols Phenylpropanoids Plants Disease Research Fields Stemona tuberosa Lour. Cancer	p38 MAPK Autophagy
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties . Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders . Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages .

HY-B0573

Propranolol hydrochloride 15+ Cited Publications	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Endocrinology	Adrenergic Receptor Bacterial
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol 15+ Cited Publications	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Adrenergic Receptor Bacterial
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-N8931

Monomethyl lithospermate Lithospermic acid monomethyl ester	Structural Classification Labiatae Source classification Samanea saman (Jacq.) Merr. Phenols Polyphenols Plants	Akt
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .

Cat. No.	Product Name	Chemical Structure

HY-107855S

DL-Mevalonolactone-d7
DL-Mevalonolactone-d₇ is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].

HY-B0573BS

Propranolol-d7

Propranolol-d₇ is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

HY-119696S

MTIC-d3
MTIC-d₃ is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].

HY-14136S

Rimonabant-d10
Rimonabant-d₁₀ is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-107855S1

DL-Mevalonolactone-d3

DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].

HY-B0573S1

Propranolol-d7 (ring-d7)

Propranolol-d₇ (ring-d₇) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

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