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CNS-penetrant

" in MedChemExpress (MCE) Product Catalog:

標的別:	5-HT Receptor (1) Akt (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (1) Antifolate (1) Apoptosis (9) ASK1 (1) ATM/ATR (2) Autophagy (8) Bacterial (1) Beta-secretase (1) c-Fms (1) Cadherin (1) Calcium Channel (1) Cannabinoid Receptor (1) Caspase (2) Collagen (1) COMT (1) COX (1) DNA Alkylator/Crosslinker (2) DNA/RNA Synthesis (5) Dopamine Receptor (3) EGFR (5) Endogenous Metabolite (3) Epigenetic Reader Domain (1) ERK (2) Eukaryotic Initiation Factor (eIF) (1) FAAH (1) Farnesyl Transferase (1) Formyl Peptide Receptor (FPR) (1) Fungal (1) FXR (1) GCGR (3) GHSR (2) Glycosidase (1) GSK-3 (2) HDAC (3) Histone Demethylase (2) iGluR (1) IKK (1) Interleukin Related (2) Isotope-Labeled Compounds (1) JNK (1) Keap1-Nrf2 (1) Ligands for Target Protein for PROTAC (1) LPL Receptor (1) LRRK2 (2) mAChR (4) MAP3K (1) MARCKS (2) mGluR (7) Mitochondrial Metabolism (2) Mitophagy (1) nAChR (4) Neurokinin Receptor (2) NF-κB (1) NOD-like Receptor (NLR) (2) P2X Receptor (2) p38 MAPK (6) Phosphodiesterase (PDE) (3) PI3K (3) PKC (1) Potassium Channel (3) Ras (1) Reactive Oxygen Species (ROS) (1) Reference Standards (6) ROCK (1) ROR (1) ROS Kinase (1) SARS-CoV (4) Serotonin Transporter (3) Sirtuin (1) Sodium Channel (1) STAT (1) STING (2) Tau Protein (1) TGF-β Receptor (1) Thyroid Hormone Receptor (1) Toll-like Receptor (TLR) (1) TREM receptor (2) Trk Receptor (1) TRP Channel (3) γ-secretase (1)
研究分野別:	Cancer (28) Cardiovascular Disease (2) Infection (16) Inflammation/Immunology (18) Metabolic Disease (18) Neurological Disease (74)
クリックケミストリー:	Alkynes (2)

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(+)-JQ-1 Maximum Cited Publications 295 Publications Verification JQ1	Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC	Neurological Disease Cancer
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .

Resveratrol 155+ Cited Publications trans-Resveratrol; SRT501	DNA/RNA Synthesis IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Resveratrol (trans-Resveratrol; SRT501) is a CNS-penetrant natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .

Substance P Maximum Cited Publications 31 Publications Verification Neurokinin P	Neurokinin Receptor Endogenous Metabolite	Infection Neurological Disease Metabolic Disease Cancer
Substance P (Neurokinin P) is a CNS-penetrant neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

Berzosertib 20+ Cited Publications VE-822; VX-970; M6620	ATM/ATR Apoptosis STING Caspase	Infection Metabolic Disease Cancer
Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .

Lonafarnib 10+ Cited Publications Sch66336	Farnesyl Transferase Ras Autophagy	Infection Neurological Disease Cancer
Lonafarnib (Sch66336) is a potent and orally active, and CNS-penetrant farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC₅₀ values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities .

Methyllycaconitine citrate 40+ Cited Publications MLA citrate	nAChR	Neurological Disease
Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .

Ozanimod 4 Publications Verification RPC-1063	LPL Receptor	Neurological Disease Inflammation/Immunology
Ozanimod (RPC-1063) is a CNS-penetrant sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P₁ and hS1P₅ receptor with EC₅₀s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .

GS-441524 25+ Cited Publications	DNA/RNA Synthesis SARS-CoV	Infection
GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .

Tersolisib 1 Publications Verification STX-478; STX-478-101; LY4064809	PI3K	Cancer
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .

Enzastaurin 10+ Cited Publications LY317615	PKC Autophagy Apoptosis	Neurological Disease Inflammation/Immunology Cancer
Enzastaurin (LY317615) is a potent, selective, and CNS-penetrant PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .

GSK805 5 Publications Verification	ROR	Inflammation/Immunology
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC₅₀ values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .

2BAct 3 Publications Verification	Eukaryotic Initiation Factor (eIF)	Neurological Disease
2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC₅₀ of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .

Ifosfamide 5+ Cited Publications	DNA Alkylator/Crosslinker	Neurological Disease Cancer
Ifosfamide is a CNS-penetrant alkylating chemotherapeutic agent with activity against a wide range of tumors.

Acetylcarnitine	Endogenous Metabolite Mitochondrial Metabolism	Neurological Disease Metabolic Disease Cancer
Acetylcarnitine is a CNS-penetrant endogenous metabolite. Acetylcarnitine shuttling links mitochondrial metabolism to histone acetylation and lipogenesis. Acetylcarnitine attenuates oxidative stress and neuroinflammation. Acetylcarnitine can be used for fatigue-associated diseases research. Acetylcarnitine can be used as a candidate diagnostic and prognostic biomarker of hepatocellular carcinoma .

IA9 2 Publications Verification human TREM-2 182-190	TREM receptor	Inflammation/Immunology
IA9 (human TREM-2 182-190) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 can be used for neuroinflammation PET imaging. IA9 can be used for Rheumatoid arthritis (RA) and neuroinflammation research .

Pemetrexed disodium hemipenta hydrate 35+ Cited Publications LY231514 disodium hemipenta hydrate	Antifolate Autophagy Apoptosis	Infection Neurological Disease Inflammation/Immunology Cancer
Pemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant antifolate, the K_i values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

Ruvonoflast NT-0796	NOD-like Receptor (NLR) Interleukin Related	Neurological Disease
Ruvonoflast (NT-0796) is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. Ruvonoflast inhibits IL-1β release in human PBMC cells with an IC₅₀ value of 0.32 nM. Ruvonoflast is an isopropyl ester that undergoes intracellular conversion to Ruvonoflast, the carboxylic acid active species. Ruvonoflast reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. Ruvonoflast is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis .

SH-4-54 15+ Cited Publications	STAT	Neurological Disease Metabolic Disease Cancer
SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively .

Zotizalkib 3 Publications Verification TPX-0131	Anaplastic lymphoma kinase (ALK)	Cancer
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC₅₀ of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC₅₀ of 0.3 nM), L1196M (IC₅₀ of 0.3 nM). Zotizalkib has strong antitumor activities .

Icotinib 5+ Cited Publications BPI-2009	EGFR	Infection Neurological Disease Metabolic Disease Cancer
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GLP-1R Antagonist 1 5 Publications Verification	GCGR	Metabolic Disease
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC₅₀ of 650 nM .

Chlorambucil 4 Publications Verification CB-1348; WR-139013	DNA Alkylator/Crosslinker	Neurological Disease Cancer
Chlorambucil (CB-1348), an orally active antineoplastic agent, is a CNS-penetrant bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .

Tolfenamic Acid 2 Publications Verification GEA 6414	COX	Infection Neurological Disease Inflammation/Immunology Cancer
Tolfenamic Acid (GEA 6414) is a CNS-penetrant non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC₅₀ of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.

Enozertinib ORIC-114	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .

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 .

MW-150 MW01-18-150SRM	p38 MAPK Autophagy	Neurological Disease Inflammation/Immunology
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K_i of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .

Fluphenazine decanoate	Dopamine Receptor	Neurological Disease
Fluphenazine decanoate is a CNS-penetrant dopamine D₂ receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research .

Buparlisib Hydrochloride 85+ Cited Publications BKM120 Hydrochloride; NVP-BKM120 Hydrochloride	PI3K Apoptosis	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a CNS-penetrant pan-class I PI3K inhibitor, with IC₅₀ of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H	EGFR	Infection Neurological Disease Metabolic Disease Cancer
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

VU0650786 2 Publications Verification	mGluR	Neurological Disease
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC₅₀ of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .

VP3.15 dihydrobromide 3 Publications Verification	Phosphodiesterase (PDE) GSK-3 Tau Protein	Cardiovascular Disease Neurological Disease Inflammation/Immunology
VP3.15 dihydrobromide is a highly potent, orally bioavailable, and CNS-penetrant PDE7-GSK3 dual inhibitor, with IC₅₀ values of 1.59 μM and 0.88 μM against PDE7 and GSK3, respectively . VP3.15 dihydrobromide elevates intracellular cAMP levels, suppresses immune responses, enhances remyelination, limits excessive tau phosphorylation, and alleviates neuroinflammation and neuronal loss. VP3.15 dihydrobromide promotes oligodendrocyte precursor cell differentiation, improves in vivo remyelination, inhibits autoimmune encephalomyelitis, and mitigates germinal matrix-intraventricular hemorrhage-related brain injury, cerebral atrophy, ventricular enlargement, and cognitive impairment. VP3.15 dihydrobromide can be used in research related to multiple sclerosis and germinal matrix-intraventricular hemorrhage .

CHDI-390576 1 Publications Verification CHDI00390576	HDAC	Cancer
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC₅₀s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .

Elunetirom MA-JD21; ABX-002	Thyroid Hormone Receptor	Neurological Disease
Elunetirom (MA-JD21 )is a TR-β selective CNS-penetrant TR-β agonist prodrug and can be used for study of major depressive disorder (MDD) .

PF-06256142 1 Publications Verification	Dopamine Receptor	Neurological Disease
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC₅₀ and K_i of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease .

LRRK2-IN-7	LRRK2	Neurological Disease
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC₅₀ of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes .

T-448	Histone Demethylase	Neurological Disease
T-448 is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC₅₀ of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons .

IA9 TFA 2 Publications Verification human TREM-2 182-190 TFA	TREM receptor	Inflammation/Immunology
IA9 TFA (human TREM-2 182-190 TFA) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 TFA can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 TFA can be used for neuroinflammation PET imaging. IA9 TFA can be used for Rheumatoid arthritis (RA) and neuroinflammation research .

Enozertinib hemihydrate ORIC-114 hemihydrate	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .

Enrupatinib EI‐1071	c-Fms Amyloid-β	Neurological Disease Cancer
Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer .

ML289 VU0463597	mGluR	Neurological Disease
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC₅₀=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

ASK1-IN-1	ASK1 MAP3K p38 MAPK	Inflammation/Immunology
ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC₅₀=138 nM; Biochemical IC₅₀=21 nM) .

Substance P TFA Maximum Cited Publications 31 Publications Verification Neurokinin P TFA	Neurokinin Receptor Endogenous Metabolite	Neurological Disease Metabolic Disease Cancer
Substance P TFA (Neurokinin P TFA) is a CNS-penetrant neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R) .

TRPV1 antagonist 3	TRP Channel	Neurological Disease
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC₅₀ of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .

Rho-Kinase-IN-2	ROCK	Neurological Disease Inflammation/Immunology Cancer
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and CNS-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC₅₀ = 3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research .

XPC-6444 1 Publications Verification	Sodium Channel	Neurological Disease
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant Na_V1.6 inhibitor (IC₅₀=41 nM for hNa_V1.6). XPC-6444 also displays potent block of Na_V1.2 (IC₅₀=125 nM). XPC-6444 shows anticonvulsant activity .

Ro 41-0960	COMT Apoptosis	Neurological Disease Cancer
Ro 41-0960 is a CNS-penetrant, orally active catechol-O-methyl transferase (COMT) inhibitor. Ro 41-0960 reduces dopamine catabolism, increases striatal dopamine and DOPAC levels, decreases striatal HVA levels, induces apoptosis, inhibits proliferation and extracellular matrix formation in uterine fibroid cells. Ro 41-0960 arrests or shrinks uterine fibroid lesions in rats. Ro 41-0960 can be used for the research of Parkinson’s disease, uterine leiomyomas, and breast cancer .

製品番号	製品名

HY-L028

CNS-Penetrant Compound Library

1,096 compounds

The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneﬁcial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.

MCE offers a unique collection of 1,096 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

HY-L093

Food Additive Library

454 compounds

Food additives are substances added to food to maintain or improve its safety, freshness, taste, texture, or appearance. All food additives used in food undergo a safety assessment, which includes rigorous testing, before they are approved, so all food additives are generally recognized as safe substances.

MCE supplies 454 approved food additives which are safe substances and can be used for drug discovery and other research.

HY-L061

Orally Active Compound Library

5,259 compounds

Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.

MCE offers a unique collection of 5,259 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.

製品番号	製品名	Target	研究分野

HY-P0201

Substance P Maximum Cited Publications 31 Publications Verification Neurokinin P	Neurokinin Receptor Endogenous Metabolite	Infection Neurological Disease Metabolic Disease Cancer
Substance P (Neurokinin P) is a CNS-penetrant neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

HY-P10136

IA9 2 Publications Verification human TREM-2 182-190	TREM receptor	Inflammation/Immunology
IA9 (human TREM-2 182-190) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 can be used for neuroinflammation PET imaging. IA9 can be used for Rheumatoid arthritis (RA) and neuroinflammation research .

HY-P10136A

IA9 TFA 2 Publications Verification human TREM-2 182-190 TFA	TREM receptor	Inflammation/Immunology
IA9 TFA (human TREM-2 182-190 TFA) is a potent, CNS-penetrant TREM-2 inhibitor. IA9 TFA can diminish the release of proinflammatory cytokines and suppress joint inflammation and damage in a Collagen (HY-P5003)-induced arthritis (CIA) mouse model. IA9 TFA can be used for neuroinflammation PET imaging. IA9 TFA can be used for Rheumatoid arthritis (RA) and neuroinflammation research .

HY-P0201A

Substance P TFA Maximum Cited Publications 31 Publications Verification Neurokinin P TFA	Neurokinin Receptor Endogenous Metabolite	Neurological Disease Metabolic Disease Cancer
Substance P TFA (Neurokinin P TFA) is a CNS-penetrant neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R) .

製品番号	製品名	構造式

HY-103586S2

GS-441524-d

GS-441524-d is the deuterium labeled GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .

製品番号	製品名		Classification

HY-15164A

Icotinib 5+ Cited Publications BPI-2009		Alkynes
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib 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-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H		Alkynes
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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