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Results for "

Brain-penetrant

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (149) Cardiovascular Disease (34) Endocrinology (16) Infection (45) Inflammation/Immunology (98) Metabolic Disease (62) Neurological Disease (468)
Click Chemistry:	Alkynes (2)

612

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17363

Dimethyl fumarate Maximum Cited Publications 56 Publications Verification	Keap1-Nrf2 Reactive Oxygen Species (ROS) HIV Autophagy Endogenous Metabolite	Infection Neurological Disease Inflammation/Immunology Cancer
Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .

HY-P9999

Trontinemab RG6102; RO-7126209	Amyloid-β	Neurological Disease
Trontinemab (RG6102) is a brain-penetrant, anti-amyloid, bispecific and humanizedized IgG1-κ antibody, targeting to Aβ plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar Aβ as well as Aβ plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1 .

HY-109566

AZD1390 5+ Cited Publications	ATM/ATR	Inflammation/Immunology Cancer
AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC₅₀ of 0.78 nM in cell .

HY-10629

LXR-623 10+ Cited Publications WAY 252623	LXR	Metabolic Disease Cancer
LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC₅₀s of 24 nM and 179 nM, respectively.

HY-N0037

Albiflorin 5+ Cited Publications	Reactive Oxygen Species (ROS)	Neurological Disease Inflammation/Immunology Cancer
Albiflorin, a major constituent contained in peony root, is a brain-penetrant monoterpene glycoside with neuroprotective effects. Albiflorin also has anti-inflammatory, antioxidant and antinociceptive effects .

HY-14781

Levomefolic acid 3 Publications Verification L-5-MTHF	Endogenous Metabolite Reactive Oxygen Species (ROS) DNA/RNA Synthesis	Infection Cancer
Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .

HY-14557

Pimavanserin 10+ Cited Publications ACP-103	5-HT Receptor	Neurological Disease
Pimavanserin is a selective, brain-penetrant, inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-W015309

Decanoic acid 4 Publications Verification	Environmental Pollutants Endogenous Metabolite iGluR Glutaminase c-Met/HGFR Tyrosinase	Neurological Disease Metabolic Disease Cancer
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .

HY-15796

GNE0877 2 Publications Verification	LRRK2	Neurological Disease
GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC₅₀ of 3 nM and a K_i of 0.7 nM. GNE0877 can be used for the research of neuroscience .

HY-10985

Marizomib 15+ Cited Publications Salinosporamide A; NPI-0052	Proteasome	Cancer
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-12947

GNE-3511 5+ Cited Publications	MAP3K	Neurological Disease
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a K_i of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .

HY-50098

Mardepodect 3 Publications Verification PF-2545920	Phosphodiesterase (PDE)	Neurological Disease Cancer
Mardepodect is a potent, selective orally active, and brain-penetrant PDE10A inhibitor with an IC₅₀ of 0.37 nM, with >1000-fold selectivity over other PDEs .

HY-134661A

Solangepras 1 Publications Verification CVN424	GPR6	Neurological Disease
CVN424 is an orally active and selective GPR6 inverse agonist with a K_i of 9.4 nM and an EC₅₀ of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research .

HY-123857

JNJ-55308942 2 Publications Verification	P2X Receptor	Neurological Disease Inflammation/Immunology
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC₅₀=10 nM, K_i=7.1 nM; rP2X7: IC₅₀=15 nM, K_i=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .

HY-P5971

TCMCB07 Mifomelatide	Melanocortin Receptor	Neurological Disease Metabolic Disease
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities .

HY-131031

KCC-07 1 Publications Verification	DNA Alkylator/Crosslinker	Cancer
KCC-07 is a potent and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity .

HY-14557A

Pimavanserin hemitartrate 10+ Cited Publications ACP-103 hemitartrate	5-HT Receptor	Neurological Disease
Pimavanserin (ACP-103) hemitartrate is a potent and brain-penetrant5-HT 2A receptor inverse agonist with pIC₅₀ and pK_i of 8.73 and 9.3, respectively.

HY-138639

PW0787 1 Publications Verification	GPR52	Neurological Disease
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC₅₀=135 nM). PW0787 suppresses psychostimulant behavior .

HY-136660

PQR626	mTOR	Neurological Disease
PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC₅₀ and K_i of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders .

HY-114379

AS2717638 2 Publications Verification	LPL Receptor	Neurological Disease Inflammation/Immunology
AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC₅₀ value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases .

HY-18163

GNE-7915 5+ Cited Publications	LRRK2	Neurological Disease
GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC₅₀ of 9 nM.

HY-134968

TTBK1-IN-1 1 Publications Verification	Tau Protein	Neurological Disease
TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor with an IC₅₀ of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies . TTBK1-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-155482

NA-184 1 Publications Verification	Proteasome	Neurological Disease
NA-184 is a selective and brain-penetrant calpain-2 inhibitor with an IC₅₀ of 134 nM for mouse calpain-2. NA-184 has weak inhibitory activity on calpain-1 (IC₅₀ of 2826 nM). NA-184 does not exhibit significant inhibition on a variety of other cysteine-, serine- or metallo-proteases. NA-184 shows significant neuroprotection and can be used for the study of traumatic brain injury (TBI) .

HY-122138

VU6010572 1 Publications Verification	mGluR	Neurological Disease
VU6010572 is a potent, selective and brain-penetrant mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

HY-145339

ARN19702	Ceramidase	Neurological Disease Inflammation/Immunology
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC₅₀ of 230 nM for human NAAA. ARN19702 has pain relief effects .

HY-B1216

Oxeladin citrate	Sigma Receptor	Cardiovascular Disease Others Neurological Disease
Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (K_i = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .

HY-12129

CP 154526 hydrochloride	CFTR	Neurological Disease
CP 154526 hydrochloride is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a K_i of 2.7 nM. CP 154526 hydrochloride shows selective for CRF1 over CRF2 (K_i = >10 μM). CP 154526 hydrochloride has anxiolytic activities .

HY-147519

ARUK3001185	Wnt	Cancer
ARUK3001185 is a potent, selective, orally active and brain-penetrant inhibitor of Notum (IC₅₀ = 6.7 nM). ARUK3001185 can restore Wnt signaling in the presence of Notum in vitro. ARUK3001185 is selective against serine hydrolases, kinases, and drug targets. ARUK3001185 can be used to research the role of Notum plays in diseases .

HY-132846

Vepafestinib TAS0953/HM06	RET Apoptosis	Cancer
Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC₅₀ value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas .

HY-110274

IP7e	Nuclear Hormone Receptor 4A/NR4A	Neurological Disease Inflammation/Immunology
IP7e is a potent, brain-penetrant and orally active Nurr1 activator with an EC₅₀ value of 3.9 nM .

HY-110130

RN-1 dihydrochloride	Histone Demethylase	Cardiovascular Disease Cancer
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC₅₀ values of 0.51 μM and 2.785 μM respectively .

HY-100366

Lu AF21934	mGluR	Neurological Disease
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC₅₀ of 500 nM for mGlu4 receptor .

HY-18081

PF 750	FAAH Autophagy	Neurological Disease Metabolic Disease
PF 750 is a selective, covalent and brain-penetrant fatty acid amide hydrolase (FAAH) inhibitor. PF 750 covalently carbamylates FAAH's catalytic serine nucleophile to inactivate the enzyme .

HY-110278

ADX71743	mGluR	Neurological Disease
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity. .

HY-12567

ML375 VU0483253	mAChR	Neurological Disease
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC₅₀s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .

HY-110184

PK-THPP	Potassium Channel	Neurological Disease
PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K ⁺ ion channel (K2P9.1 or TASK-3) blocker with IC₅₀s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K ⁺ channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders .

HY-117764

LSP4-2022	mGluR	Neurological Disease
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC₅₀ of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .

HY-12959A

Repinotan hydrochloride BAY x 3702	5-HT Receptor	Neurological Disease
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with K_i values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .

HY-106770

Esuprone	Monoamine Oxidase	Neurological Disease
Esuprone is a brain-penetrant, orally active and selective MAO A inhibitor with an IC₅₀ of 7.3 nM. Esuprone can be used for neurological research .

HY-111520

NVS-SM2	DNA/RNA Synthesis	Neurological Disease
NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC₅₀ of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research .

HY-161903

Progranulin modulator-3	Neurotensin Receptor	Neurological Disease
Progranulin modulator-3 (compd C40) is a brain-penetrant and orally active progranulin (PGRN) inducer. Progranulin modulator-3 can be used for neurological research .

HY-116480

LY593093	mAChR	Neurological Disease
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC₅₀ of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .

HY-144266

TP-060 Glucosylceramide synthase-IN-1	Glucosylceramide Synthase (GCS)	Neurological Disease Metabolic Disease
Glucosylceramide synthase-IN-1 (T-036), a chemical probe, a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC₅₀s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research .

HY-W709856

Dodeca-2E,4E,8Z,10Z/E-N-tetraenoic acid isobutylamide	Influenza Virus	Infection
Dodeca-2E,4E,8Z,10Z/E-N-tetraenoic acid isobutylamide is a brain-penetrant substance and the main alkamide in Echinacea preparations, which might be used for research of common cold and various upper respiratory infections .

HY-174066

SI-W052	mTOR Autophagy Interleukin Related	Neurological Disease Inflammation/Immunology
SI-W052 is an orally active, brain-penetrant and selective small-molecule inhibitor targeting mTOR and TEX264. SI-W052 activates autophagy by inhibiting mTOR phosphorylation and enhances TEX264 expression to promote ER turnover, suppressing LPS-induced release of inflammatory factors (TNF-α, IL-6). SI-W052 is promising for research of Alzheimer’s disease (AD)-associated neuroinflammation .

HY-133813A

Apovincaminic acid hydrochloride salt	Drug Metabolite	Neurological Disease
Apovincaminic acid hydrochloride salt is an orally active and brain-penetrant main active metabolite of Vinpocetine (VP). Apovincaminic acid hydrochloride salt exerts a neuroprotective type of action .

HY-144267

Glucosylceramide synthase-IN-2	Glucosylceramide Synthase (GCS)	Neurological Disease Metabolic Disease
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC₅₀s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research .

HY-12981

RG7713 2 Publications Verification RO5028442	Vasopressin Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
RG7713 (RO5028442) is a highly potent, selective and brain-penetrant Vasopressin 1a (V1a) receptor antagonist with K_is of 1 nM (hV1a) and 39 nM (mV1a).

HY-34222

7-Deazaguanine	DYRK	Cancer
7-Deazaguanine (Compound 1) is a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor. 7-Deazaguanine is promising for research of cancers and Down’s syndrome .

HY-139144

YM-08	Sirtuin HSP	Neurological Disease Cancer
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC₅₀ of 19.9 μM. YM-08 also is inhibitor of Hsp70 .

Cat. No.	Product Name	Type

HY-12495A

ISRIB

25+ Cited Publications

Biochemical Assay Reagents

ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .

HY-D0714

Tetrazolium Red

5+ Cited Publications

2,3,5-Triphenyltetrazolium chloride; TPTZ; TTC

Biochemical Assay Reagents

Tetrazolium Red (2,3,5-Triphenyltetrazolium chloride; TTC) is a not brain-penetrant, colorless, water-soluble dye that is reduced by mitochondrial enzymes to a deep red, water-insoluble compound (formazan) mainly in the mitochondria of living cells. Tetrazolium Red is used to observe the activity of dehydrogenase, and it turns colorless to red when exposed to hydrogen. Tetrazolium Red distinguishes between surviving and infarcted brain tissue after stroke. Tetrazolium Red has been used to stain heart tissue to measure the extent of acute lesions and also used to stain brain tissue to detect the size of the infarcted area. The absorption wavelength of Tetrazolium Red is 570 nm .

Cat. No.	Product Name	Target	Research Area

HY-P1363

β-Amyloid (1-42), human TFA 20+ Cited Publications Amyloid β-peptide (1-42) (human) TFA	Amyloid-β	Neurological Disease
β-Amyloid (1-42) (Amyloid β-peptide (1-42), human TFA, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human TFA remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human TFA, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .

HY-P1363A

β-Amyloid (1-42), human 20+ Cited Publications Amyloid β-peptide (1-42) (human)	Amyloid-β	Neurological Disease
β-Amyloid (1-42) (Amyloid β-peptide (1-42)), human, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .

HY-P1363B

β-Amyloid (1-42), human, HFIP-treated 20+ Cited Publications	Amyloid-β	Neurological Disease
β-Amyloid (1-42), human, HFIP-treated, a 42-amino acid peptide that has been treated with HFIP from β-Amyloid (1-42), human (HY-P1363A), is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human, HFIP-treated remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, HFIP-treated, after being dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4°C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37°C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .

HY-P1061

Colivelin Maximum Cited Publications 92 Publications Verification	STAT Amyloid-β	Neurological Disease
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro . Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease . Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

HY-P1061A

Colivelin TFA Maximum Cited Publications 92 Publications Verification	STAT Amyloid-β Apoptosis	Neurological Disease
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro . Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease . Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury .

HY-P5971

TCMCB07 Mifomelatide	Melanocortin Receptor	Neurological Disease Metabolic Disease
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities .

HY-P3538

Corticotropin-releasing factor (Sheep) CRH (Sheep)	Peptides	Neurological Disease
Corticotropin-releasing factor (CRH) (Sheep) is a brain-penetrant hypothalamic releasing factor and a peptide hormone with analgesic and arousal-inducing activity. Corticotropin-releasing factor (Sheep) mediates stress effects, including stress-induced analgesia. Corticotropin-releasing factor (Sheep) increases wakefulness, reduces slow wave sleep, alters EEG frequency content, stimulates ACTH and β-endorphin release, activates locomotor activity. Corticotropin-releasing factor (Sheep) can be used for the research of neurological disease .

HY-P10862

AH-D peptide	Exosomes Virus Protease	Infection Cancer
AH-D peptide is a brain-penetrant antiviral agent disrupting highly curved lipid membranes. AH-D peptide exhibits broad-spectrum antiviral activity against ZIKV, Dengue virus, Chikungunya virus, yellow fever virus and Japanese encephalitis virus, with IC₅₀ values of 11.9, 12.5, 35.7, 206 and 136 nM, respectively. AH-D peptide reduces the viral load in the brain, suppresses inflammation, protects neurons, and does not damage the blood brain barrier. AH-D peptide restores antitumor immunity by decreasing circulating PD-L1 ⁺ exosomes, reducing intratumoral immunosuppressive cells (regulatory T cells, myeloid-derived suppressor cells), and enhancing T cell function. AH-D peptide inhibits membrane-enveloped viruses and cancer cell metastasis in vivo. AH-D peptide exhibits no immunogenicity and has negligible effects on normal tissues. AH-D peptide can be used for research in Zika virus and other mosquito-borne viruses, cancer immunotherapy and metastasis .

HY-153963

PF-06655075	Oxytocin Receptor	Endocrinology
PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .

HY-101230

ICI 174864	Opioid Receptor	Neurological Disease
ICI 174864 is a selective and brain-penetrant δ-opioid receptor antagonist with K_e values of 22.0 nM to 30.6 nM at δ-opioid receptor in mouse vas deferens. ICI 174864 selectively blocks biological effects mediated by the δ-opioid receptor agonist DPDPE (HY-P1334) after central administration. ICI 174864 reverses hypotension in rats with endotoxic shock and inhibits acetic acid-induced writhing in mice. ICI 174864 can be used for the research of opioid receptor subtypes, endotoxic hypotension and analgesic pathways .

HY-P5971A

TCMCB07 TFA	Melanocortin Receptor	Metabolic Disease
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia .

HY-P1363S1

β-Amyloid (1-42), human, Ala(13C3,15N) TFA	Isotope-Labeled Compounds Amyloid-β	Neurological Disease
β-Amyloid (1-42), human, Ala( ¹³C₃, ¹⁵N) TFA is the ¹³C and ¹⁵N-labeled β-Amyloid (1-42), human (HY-P1363A). β-Amyloid (1-42) (Amyloid β-peptide (1-42)), human, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .

HY-P10824

RI-OR2-TAT	Amyloid-β	Neurological Disease
RI-OR2-TAT is a brain-penetrant inhibitor of β-Amyloid oligomerization, which is produced by adding the HIV protein transduction domain TAT to RI-OR2. RI-OR2-TAT binds to Aβ42 fibrils with a K_d value of 58-125 nM. RI-OR2-TAT reduces Aβ aggregation and plaque levels, reduces activation of microglia and oxidative damage, and increases the number of young neurons in the dentate gyrus .

HY-153963A

PF-06655075 TFA	Oxytocin Receptor	Endocrinology
PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response .

Cat. No.	Product Name	Target	Research Area	Image

HY-P9999

Trontinemab RG6102; RO-7126209	Amyloid-β	Neurological Disease
Trontinemab (RG6102) is a brain-penetrant, anti-amyloid, bispecific and humanizedized IgG1-κ antibody, targeting to Aβ plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar Aβ as well as Aβ plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1 .

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a *brain-penetrant* and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .

HY-P99403

Refanezumab GSK249320	Inhibitory Antibodies	Neurological Disease
Refanezumab (GSK249320) is a brain-penetrant IgG1-type humanized monoclonal antibody directed against myelin-associated glycoprotein (MAG). Refanezumab binds to MAG and blocks MAG-mediated inhibition of axonal regeneration. Refanezumab has the potential for the enhancement of recovery of function poststroke .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-17363

Dimethyl fumarate Maximum Cited Publications 56 Publications Verification	Infection Natural Products Neurological Disease Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Keap1-Nrf2 Reactive Oxygen Species (ROS) HIV Autophagy Endogenous Metabolite
Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .

HY-N0037

Albiflorin 5+ Cited Publications	Structural Classification Other Monoterpenes Paeonia lactiflora Pall. Classification of Application Fields Terpenoids Plants Paeoniaceae Inflammation/Immunology Disease Research Fields Source Classification	Reactive Oxygen Species (ROS)
Albiflorin, a major constituent contained in peony root, is a brain-penetrant monoterpene glycoside with neuroprotective effects. Albiflorin also has anti-inflammatory, antioxidant and antinociceptive effects .

HY-14781

Levomefolic acid 3 Publications Verification L-5-MTHF	Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification Cancer	Endogenous Metabolite Reactive Oxygen Species (ROS) DNA/RNA Synthesis
Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .

HY-W015309

Decanoic acid 4 Publications Verification	Structural Classification Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Biological Pesticide Research Source Classification Agricultural Research	Environmental Pollutants Endogenous Metabolite iGluR Glutaminase c-Met/HGFR Tyrosinase
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .

HY-N2364

Arecoline 5 Publications Verification	Structural Classification Neurological Disease Classification of Application Fields Areca catechu L. Metabolic Disease Plants Infection Alkaloids Piperidine Alkaloids Palmae Inflammation/Immunology Disease Research Fields Source Classification	mAChR nAChR
Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress .

HY-10985

Marizomib 15+ Cited Publications Salinosporamide A; NPI-0052	Marine natural products Marine microorganism Source Classification	Proteasome
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively) .

HY-B0489

Arecoline hydrobromide 5 Publications Verification methyl 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylate hydrobromide	Structural Classification Neurological Disease Classification of Application Fields Areca catechu L. Metabolic Disease Plants Infection Alkaloids Other Alkaloids Palmae Inflammation/Immunology Disease Research Fields Source Classification	mAChR nAChR
Arecoline hydrobromide, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .

HY-110252

Salvinorin B	Terpenoids Labiatae Encelia stenophylla Greene Diterpenoids Plants Source Classification	Opioid Receptor
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC₅₀ of 248 nM and K_i of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .

HY-N2072

Crocetin 3 Publications Verification Transcrocetin; trans-Crocetin	Structural Classification Classification of Application Fields Terpenoids Diterpenoids Lridaceae Plants Crocus sativus L. Endogenous metabolite Disease Research Fields Source Classification Cancer	iGluR Apoptosis COX p38 MAPK
Crocetin (Transcrocetin) is an aglycone of crocin. Crocetin is an orally active and brain-penetrant. Crocetin shows strong NMDA receptor affinity and channel opening activity. Crocetin can downregulate the proinflammatory cytokines and COX-2 exoression. Crocetin can inhibit apoptosis and activation of MAPK. Crocetin can delay delays brain and body aging. Crocetin can be used for the researches of cancer, neurological disease and inflammation, such as cervical cancer and ischemia .

HY-D0186

2'-Deoxyuridine 3 Publications Verification	Infection Natural Products Immune System Disorder Microorganisms Classification of Application Fields Disease markers Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite Thymidylate Synthase
2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .

HY-B0979

Lobeline hydrochloride 1 Publications Verification α-Lobeline hydrochloride; L-Lobeline hydrochloride	Alkaloids Campanulaceae Pyridine Alkaloids Plants Lobelia chinensis Lour. Source Classification	nAChR Dopamine Transporter
Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .

HY-14602

Tramiprosate 2 Publications Verification Homotaurine; 3-Amino-1-propanesulfonic acid	Microorganisms other families Classification of Application Fields Ketones, Aldehydes, Acids Plants Disease Research Fields Source Classification Cancer	Amyloid-β
Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects .

HY-59291

Levacetylleucine N-Acetyl-L-leucine	Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Amino Acid Derivatives
Levacetylleucine (N-acetyl-L-leucine), an orally bioavailable and brain-penetrant compound, is an acetylated derivative of amino acid Leucine. Levacetylleucine is the active form of N-acetyl-leucine (NAL). Levacetylleucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. Levacetylleucine also potentially improves ameliorates lysosomal and metabolic dysfunction. Levacetylleucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. Levacetylleucine is promising for research of neurological manifestations of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention .

HY-N2392

Kukoamine A 1 Publications Verification	Cardiovascular Disease Alkaloids Structural Classification other families Classification of Application Fields Other Alkaloids Phenols Polyphenols Plants Disease Research Fields Source Classification	Parasite Lipoxygenase Opioid Receptor Apoptosis Autophagy Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor PGE synthase COX
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE₂, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .

HY-N1983

Caudatin 1 Publications Verification	Structural Classification Classification of Application Fields Asclepiadaceae Cynanchum otophyllum Schneid． Cynanchum auriculatum Royle ex Wight Plants Disease Research Fields Steroids Source Classification Cancer	Apoptosis Autophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism PARP Caspase Bcl-2 Family VEGFR FAK WDR5 p38 MAPK JNK PPAR
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .

HY-N0430

Coptisine Coptisin	Alkaloids Structural Classification Classification of Application Fields Coptis chinensis Franch. Ranunculaceae Metabolic Disease Quinoline Alkaloids Plants Disease Research Fields Source Classification	Indoleamine 2,3-Dioxygenase (IDO) NF-κB p38 MAPK PI3K Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism DNA/RNA Synthesis ROCK LDLR
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a K_i of 5.8 μM and an IC₅₀ of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .

HY-N0430A

Coptisine Sulfate 5 Publications Verification	Alkaloids Structural Classification Chelidonium majus Classification of Application Fields Metabolic Disease Quinoline Alkaloids Plants Disease Research Fields Papaveraceae Source Classification	Indoleamine 2,3-Dioxygenase (IDO) NF-κB p38 MAPK PI3K Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism DNA/RNA Synthesis ROCK LDLR
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a K_i of 5.8 μM and an IC₅₀ of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .

HY-N2125

Parishin C	Structural Classification Gastrodia elata Bl. Orchidaceae Phenols Plants Source Classification	5-HT Receptor iGluR Caspase Interleukin Related TNF Receptor SOD NF-κB
Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC₅₀ of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis .

HY-W709856

Dodeca-2E,4E,8Z,10Z/E-N-tetraenoic acid isobutylamide	Alkaloids Other Alkaloids Plants Compositae Echinacea angustifolia DC. Source Classification	Influenza Virus
Dodeca-2E,4E,8Z,10Z/E-N-tetraenoic acid isobutylamide is a brain-penetrant substance and the main alkamide in Echinacea preparations, which might be used for research of common cold and various upper respiratory infections .

HY-W009300

4-Hydroxyestrone 1 Publications Verification 4-OHE1	Structural Classification Animals Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification	Endogenous Metabolite Estrogen Receptor/ERR Sirtuin MDM-2/p53 PDI Ferroptosis Reactive Oxygen Species (ROS)
4-Hydroxyestrone (4-OHE1) is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .

HY-W674241A

4-Ethylphenyl sulfate sodium	Structural Classification Natural Products Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite Apoptosis Bcl-2 Family Reactive Oxygen Species (ROS)
4-Ethylphenyl sulfate sodium is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate sodium downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate sodium induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate sodium impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate sodium alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice .

HY-17363R

Dimethyl fumarate (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Keap1-Nrf2 Reactive Oxygen Species (ROS) HIV Autophagy Endogenous Metabolite
Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .

HY-B1423

Lobeline α-Lobeline; L-Lobeline	Alkaloids Other Alkaloids Campanulaceae Plants Lobelia chinensis Lour. Source Classification	nAChR Dopamine Transporter
Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation .

HY-N2072R

Crocetin (Standard) Transcrocetin (Standard); trans-Crocetin (Standard)	Structural Classification Terpenoids Diterpenoids Lridaceae Plants Crocus sativus L. Endogenous metabolite Source Classification	iGluR Reference Standards Apoptosis COX p38 MAPK
Crocetin (Standard) (TransCrocetin (Standard) ) is an aglycone of crocin. Crocetin (Standard) is orally active and brain-penetrant. Crocetin (Standard) shows strong NMDA receptor affinity and channel opening activity. Crocetin (Standard) can downregulate the proinflammatory cytokines and COX-2 exoression. Crocetin (Standard) can inhibit apoptosis and activation of MAPK. Crocetin (Standard) can delay delays brain and body aging. Crocetin (Standard) can be used for the researches of cancer, neurological disease and inflammation, such as cervical cancer and ischemia .

HY-N6685

3-Acetyldeoxynivalenol 3-AcDON; 3-ADON	Cardiovascular Disease Structural Classification Microorganisms Classification of Application Fields Terpenoids Sesquiterpenes Disease Research Fields Source Classification	Endogenous Metabolite Interleukin Related
3-Acetyldeoxynivalenol (3-AcDON; 3ADON), a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a brain-penetrant Fusarium mycotoxin. 3-Acetyldeoxynivalenol induces mRNA expression and production of inflammatory chemokine IL-8 in intestinal cells .

HY-D0186R

2'-Deoxyuridine (Standard)	Structural Classification Natural Products Immune System Disorder Microorganisms Disease markers Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite Thymidylate Synthase
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) . In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine . Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min . In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain . 2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .

HY-13906

Largazole (+)-Largazole	Structural Classification Natural Products Microorganisms Source Classification	HDAC
Largazole ((+)-Largazole) is a potent, selective, orally active and brain-penetrant class I HDAC inhibitor found in marine cyanobacteria. Largazole shows an IC₅₀ of 0.07 nM for HDAC2. Largazole releases its active form Largazole thiol (HY-170890) after hydrolysis. Largazole has a strong inhibitory effect on SF-268, SF-295 and SH-SY5Y cells, with IC₅₀ values of 62, 68 and 102 nM respectively Largazole can upregulate the tumor suppressor gene Pax6 to inhibit the proliferation, invasion and colony formation of glioblastoma cells. Largazole can significantly upregulated brain-derived neurotrophic factor BDNF, neuronal transcription factor Pax6, and μ-opioid receptor gene Oprm1. Largazole exerts antitumor and neuroprotective effects. Largazole can be used for researches of Glioblastoma and Alzheimer’s disease .

HY-N1983R

Caudatin (Standard)	Structural Classification Asclepiadaceae Cynanchum otophyllum Schneid． Cynanchum auriculatum Royle ex Wight Plants Steroids Source Classification	Reference Standards Apoptosis Autophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism PARP Caspase Bcl-2 Family VEGFR FAK WDR5 p38 MAPK JNK PPAR
Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .

HY-128420

Lobeline sulfate α-Lobeline sulfate; L-Lobeline sulfate	Alkaloids other families Pyridine Alkaloids Plants Endogenous metabolite Source Classification	nAChR Dopamine Transporter
Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation .

HY-B0979R

Lobeline hydrochloride (Standard) α-Lobeline hydrochloride (Standard); L-Lobeline hydrochloride (Standard)	Alkaloids Structural Classification Campanulaceae Pyridine Alkaloids Plants Lobelia chinensis Lour. Source Classification	Reference Standards nAChR Dopamine Transporter
Lobeline (hydrochloride) (Standard) is the analytical standard of Lobeline (hydrochloride). This product is intended for research and analytical applications. Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .

HY-N10183

Crocin-4	Crocus sativus Linn. Iridaceae Terpenoids Diterpenoids Plants Source Classification	Reactive Oxygen Species (ROS)
Crocin-4, a carotenoid constituent of saffron, is a potent and brain-penetrant antioxidant agent. Crocin-4 can inhibit the aggregation and the concomitant deposition of Aβ fibrils in the brain. Crocin-4 can be used for the research of Alzheimer's Disease. Crocin-4 also exhibits antitumor and anti-inflammatory activities .

HY-B0489R

Arecoline hydrobromide (Standard) methyl 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylate hydrobromide (Standard)	Alkaloids Structural Classification Areca catechu L. Other Alkaloids Palmae Plants Source Classification	Reference Standards mAChR nAChR
Arecoline hydrobromide (Standard) is the analytical standard of Arecoline hydrobromide. This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .

HY-13764A

dl-Tetrandrine	Alkaloids Stephania japonica var. discolor (Blume) Forman Plants Menispermaceae Alkaloid Dimers Source Classification	Calcium Channel
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca ²⁺ influx with an IC₅₀ value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal .

HY-W015309R

Decanoic acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards iGluR Tyrosinase c-Met/HGFR Glutaminase
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .

HY-B0489A

Arecoline hydrochloride	Structural Classification Neurological Disease Classification of Application Fields Areca catechu L. Metabolic Disease Plants Infection Alkaloids Other Alkaloids Palmae Inflammation/Immunology Disease Research Fields Source Classification	mAChR nAChR
Arecoline hydrochloride, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrochloride exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrochloride also can induce oxidative stress .

HY-14602R

Tramiprosate (Standard) Homotaurine (Standard); 3-Amino-1-propanesulfonic acid (Standard)	Structural Classification Microorganisms other families Ketones, Aldehydes, Acids Plants Source Classification	Reference Standards Amyloid-β
Tramiprosate (Standard) is the analytical standard of Tramiprosate. This product is intended for research and analytical applications. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects .

HY-N6685R

3-Acetyldeoxynivalenol (Standard) 3-AcDON (Standard); 3-ADON (Standard)	Structural Classification Microorganisms Terpenoids Sesquiterpenes Source Classification	Reference Standards Endogenous Metabolite Interleukin Related
3-Acetyldeoxynivalenol (3-AcDON; 3ADON) (Standard) is the analytical standard of 3-Acetyldeoxynivalenol (HY-N6685). This product is intended for research and analytical applications. 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a brain-penetrant Fusarium mycotoxin. 3-Acetyldeoxynivalenol induces mRNA expression and production of inflammatory chemokine IL-8 in intestinal cells .

HY-N9503

Carvacryl acetate	Structural Classification Natural Products Labiatae Launaea mucronata (Forssk.) Muschl. Plants Source Classification	TRP Channel Na+/K+ ATPase Parasite
Carvacryl acetate is an orally active and brain-penetrant TRPA1 receptor activator and Na ⁺/K ⁺-ATPase activator. Carvacryl acetate modulates GABAergic signaling, alters hippocampal GABA and glutamine levels, reduces lipid peroxidation and nitrite formation, scavenges hydroxyl radicals, and boosts glutathione and antioxidant enzyme activity. Carvacryl acetate inhibits Haemonchus contortus larval hatching, development, adult motility, and fecal egg counts, and induces adult worm structural damage. Carvacryl acetate can be used for the research of intestinal mucositis, gastrointestinal nematode infection, epilepsy, and neurodegenerative diseases .

HY-N2125R

Parishin C (Standard)	Structural Classification Gastrodia elata Bl. Orchidaceae Phenols Plants Source Classification	Reference Standards 5-HT Receptor iGluR Caspase Interleukin Related TNF Receptor SOD NF-κB
Parishin C (Standard) is the analytical standard of Parishin C (HY-N2125). This product is intended for research and analytical applications. Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC₅₀ of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis .

HY-113371R

2-Methylcitric acid (Standard) Methylcitric acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Disease markers Endocrine diseases Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
Omeprazole (sodium) (Standard) is the analytical standard of Omeprazole (sodium). This product is intended for research and analytical applications. Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .

Cat. No.	Product Name	Chemical Structure

HY-B0590S

Tetrabenazine-d6

Tetrabenazine-d₆ (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-W015309S1

Decanoic acid-d19
Decanoic acid-d₁₉9 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects .

HY-14781S1

Levomefolic acid-13C,d3
Levomefolic acid- ¹³C,d₃ is the deuterium labeled Levomefolic acid (HY-14781) . Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .

HY-17363S1

Dimethyl fumarate-d2

Dimethyl fumarate-d₂ is the deuterium labeled Dimethyl fumarate . Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .

HY-W266188

Decanoic acid-13C

Decanoic acid- ¹³C is the ¹³C-labeled Decanoic acid (HY-W015309). Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .

HY-W015309S3

Decanoic acid-d5
Decanoic acid-d₅ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects .

HY-14602S

Tramiprosate-d6
Tramiprosate-d₆ is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects .

HY-B0688S2

Dapsone-13C12

Dapsone- ¹³C₁₂ is the ¹³C₁₂ labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .

HY-W015309S

Decanoic acid-d3
Decanoic acid-d₃ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects .

HY-14781S2

Levomefolic acid-13C5
Levomefolic acid- ¹³C₅ is the ¹³C labeled Levomefolic acid . Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .

HY-11063S

Fingolimod-d4
Fingolimod-d₄ is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC₅₀ of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .

HY-B0688S

Dapsone-d8
Dapsone-d₈ is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases .

HY-14781S3

Levomefolic acid-d3
Levomefolic acid-d₃ (L-5-MTHF-d₃) is deuterium labeled Levomefolic acid. Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements .

HY-175483S

TrkB activator-1

TrkB activator-1 is a specific, orally active and brain-penetrant tropomyosin receptor kinase B (TrkB) activator. TrkB activator-1 shows potent antidepressant effects through activation of the activates the BDNF (brainderived neurotrophic factor)-Tropomyosin-related kinase B (TrkB)-CREB (cAMP response element binding protein) signaling aixs. TrkB activator-1 increaes neuroplasticity. TrkB activator-1 can be used for the research of neurological disease, such as depression .

HY-W707863

Lercanidipine-d3

Lercanidipine-d₃ is the deuterium labeled Lercanidipine (HY-B0612). Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC₅₀ of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research .

HY-W778990

2-Deoxyuridine-1,2,3,4,5-13C5

2-Deoxyuridine-1,2,3,4,5- ¹³C₅ is the ¹³C-labeled 2'-Deoxyuridine (HY-D0186). 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .

HY-13662BS

(R)-Lansoprazole-d4
(R)-Lansoprazole-d₄ is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .

HY-B0688S1

Dapsone-d4

Dapsone-d₄ is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .

HY-P1363S1

β-Amyloid (1-42), human, Ala(13C3,15N) TFA

β-Amyloid (1-42), human, Ala( ¹³C₃, ¹⁵N) TFA is the ¹³C and ¹⁵N-labeled β-Amyloid (1-42), human (HY-P1363A). β-Amyloid (1-42) (Amyloid β-peptide (1-42)), human, a 42-amino acid peptide that has not been treated with HFIP, is a brain-penetrant amyloid protein fragment, which can be used in research on Alzheimer's disease and Down’s syndrome. β-Amyloid (1-42), human remaining as a monomer exhibits antioxidant and neuroprotective effects. β-Amyloid (1-42), human, after being monomericized by HFIP and dissolved in DMSO to form the stock solution, on the one hand, can form soluble oligomers (AβOs) when incubated at 4 °C, which have synaptic toxicity and neurotoxicity; on the other hand, it can be incubated at 37 °C to form insoluble fibrils, with lower neurotoxicity, and participating in the oxidative damage process. Aβ42 oligomers bind to various neuronal surface receptors (such as PrPc, mGluR5, NMDA receptors, etc.), triggering oxidative stress, calcium homeostasis imbalance, and synaptic toxicity via activating downstream signaling pathways, leading to neuronal dysfunction and death .

HY-W015309S2

Decanoic acid-d2
Decanoic acid-d₂ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects .

HY-B0534S1

Moclobemide-d4
Moclobemide-d₄ is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC₅₀ of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.

HY-11063S1

Fingolimod-d4 hydrochloride
Fingolimod-d₄ (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC₅₀ of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant .

HY-B0534S

Moclobemide-d8
Moclobemide-d₈ (Ro111163-d₈) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC₅₀ of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.

HY-N6685S1

3-Acetyldeoxynivalenol-13C17
3-Acetyldeoxynivalenol (3-AcDON; 3ADON)- ¹³C₁₇ is the ¹³C labeled 3-Acetyldeoxynivalenol (HY-N6685). 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a brain-penetrant Fusarium mycotoxin. 3-Acetyldeoxynivalenol induces mRNA expression and production of inflammatory chemokine IL-8 in intestinal cells .

HY-B0568S

Deferiprone-d3

Deferiprone-d₃ is the deuterium labeled Deferiprone (HY-B0568). Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .

HY-17383S

Levomefolate-13C5 calcium

Levomefolate- ¹³C₅ calcium)is the ¹³C-labeled Levomefolate calcium (HY-17383). Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia .

HY-B0590S3

Tetrabenazine-d7

Tetrabenazine-d₇ (TBZ-d₇-d₇) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .

HY-W013150S

Alpidem-d14

Alpidem-d₁₄ is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC₅₀ of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC₅₀ of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.

HY-W009300S

4-Hydroxyestrone-d4

4-Hydroxyestrone (4-OHE1)-d₄ is the deuterium labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .

HY-W017540S

Cyclocreatine-13C3

Cyclocreatine- ¹³C₃ is the ¹³C-labeled Cyclocreatine (HY-W017540). Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .

HY-W009300S1

4-Hydroxyestrone-13C6

4-Hydroxyestrone (4-OHE1)- ¹³C₆ is a ¹³C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .

HY-W027553S1

Ipidacrine-d9

Ipidacrine-d₉ (NIK-247-d₉ (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

HY-B0688S3

Dapsone-15N2

Dapsone- ¹⁵N₂ (4,4′-Diaminodiphenyl sulfone- ¹⁵N₂) is ¹⁵N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .

Cat. No.	Product Name		Classification

HY-142035

N-Propargylglycine 1 Publications Verification		Alkynes
N-Propargylglycine is a brain-penetrant and orally active PRODH inhibitor. N-Propargylglycine covalently modifies enzyme-bound FAD and active site lysine, causing enzyme structural distortion, protein decay, and irreversible inhibition of proline and 4-hydroxyproline catabolism. N-Propargylglycine induces UPRmt, upregulates mitochondrial chaperones and YME1L1, enhances mitochondrial proteostasis, blocks astrocytic L-proline consumption, and abolishes L-proline’s ATP-maintaining and viability-protective effects. N-Propargylglycine stimulates neural processes, increases brain proline, hydroxyproline, and sarcosine levels, partially normalizes Huntington’s disease whole brain transcriptomes. N-Propargylglycine reduces hyperoxaluria, prevents calcium oxalate stone formation, reduces kidney tubular damage, and restores weight and survival in Grhpr knockout mice. N-Propargylglycine can be used for the research of breast cancer, neurodegenerative disorders, Huntington’s disease, and primary hyperoxaluria type 2 .

HY-178164

HBS-101		Alkynes
HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (K_D = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC) .

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