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Blood-brain barrier penetrant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Amyloid-β (2) Apoptosis (1) Autophagy (1) Calcium Channel (1) Cholinesterase (ChE) (3) DNA/RNA Synthesis (2) Dopamine Receptor (6) ERK (1) GPR52 (1) Histamine Receptor (3) iGluR (1) Isotope-Labeled Compounds (2) MAGL (1) MAP3K (1) Monoamine Oxidase (2) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) Opioid Receptor (4) Oxytocin Receptor (1) p38 MAPK (1) Raf (1) Reactive Oxygen Species (1) Sigma Receptor (2) Topoisomerase (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (6) Endocrinology (2) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (24)

By Targets:

5-HT Receptor (1)

Amyloid-β (2)

Apoptosis (1)

Autophagy (1)

Calcium Channel (1)

Cholinesterase (ChE) (3)

DNA/RNA Synthesis (2)

Dopamine Receptor (6)

ERK (1)

GPR52 (1)

Histamine Receptor (3)

iGluR (1)

Isotope-Labeled Compounds (2)

MAGL (1)

MAP3K (1)

Monoamine Oxidase (2)

Neurokinin Receptor (1)

Neuropeptide Y Receptor (1)

Opioid Receptor (4)

Oxytocin Receptor (1)

p38 MAPK (1)

Raf (1)

Reactive Oxygen Species (1)

Sigma Receptor (2)

Topoisomerase (1)

Vasopressin Receptor (1)

By Research Areas:

Cancer (6)

Endocrinology (2)

Inflammation/Immunology (2)

Metabolic Disease (1)

Neurological Disease (24)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15722

SB-222200 2 Publications Verification	Neurokinin Receptor	Neurological Disease Endocrinology
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .

HY-15976

P7C3 5+ Cited Publications	Others	Neurological Disease
P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease .

HY-144610

Mu opioid receptor antagonist 5	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC₅₀ value of 1.14 nM and a K_i value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .

HY-144607

Mu opioid receptor antagonist 2	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a K_i of 0.37 nM and an EC₅₀ of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .

HY-117501

Dexchlorpheniramine	Histamine Receptor	Inflammation/Immunology
Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies .

HY-111455

LP-211 1 Publications Verification	5-HT Receptor	Neurological Disease
LP-211 is a selective and blood−brain barrier penetrant 5-HT₇ receptor agonist, with a K_i of 0.58 nM, with high selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM).

HY-10328

Neflamapimod Maximum Cited Publications 9 Publications Verification VX-745	p38 MAPK Autophagy	Inflammation/Immunology
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC₅₀ for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.

HY-147953

MAO-B-IN-13	Monoamine Oxidase	Neurological Disease
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC₅₀ value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease .

HY-134189

EST73502	Opioid Receptor Sigma Receptor	Neurological Disease
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .

HY-134189A

EST73502 monohydrochloride	Sigma Receptor Opioid Receptor	Neurological Disease
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .

HY-136731

APE1-IN-1	DNA/RNA Synthesis	Cancer
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC₅₀ value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .

HY-33009

AS057278	Others	Neurological Disease
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC₅₀ value of 0.91 μM and EC₅₀ of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia .

HY-150791

FLDP-5	Reactive Oxygen Species DNA/RNA Synthesis	Cancer
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .

HY-17387

(-)-Huperzine A 3 Publications Verification Huperzine A	Cholinesterase (ChE) Apoptosis iGluR	Neurological Disease
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .

HY-150639

Everafenib	Raf	Cancer
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of ^V600EBRAF melanoma cell lines with IC₅₀ values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .

HY-147395

GPR52 agonist-1	GPR52	Neurological Disease
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC₅₀ value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .

HY-137466

ARN-21934	Topoisomerase	Cancer
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC₅₀ of 2 μM as compared to the anticancer agent Etoposide (IC₅₀=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .

HY-17355

Pramipexole dihydrochloride 4 Publications Verification	Dopamine Receptor	Neurological Disease
Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with K_is of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D₂, D₃ and D₄ receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .

HY-B0410

Pramipexole 4 Publications Verification	Dopamine Receptor	Neurological Disease
Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with K_is of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D₂, D₃ and D₄ receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .

HY-B0410A

Pramipexole dihydrochloride hydrate 4 Publications Verification
Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with K_is of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D₂, D₃ and D₄ receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .

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-17355S

Pramipexole-d7 dihydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Pramipexole-d₇ (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

HY-17355S1

Pramipexole-d5 dihydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Pramipexole-d₅ (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

HY-B0410S1

Pramipexole-d5	Dopamine Receptor	Neurological Disease
Pramipexole-d₅ is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].

HY-163202

MAGL-IN-13	MAGL Calcium Channel	Neurological Disease Cancer
MAGL-IN-13 (compound (3R, 4S) - 5v) is a selective, irreversible inhibitor for MAGL,with IC₅₀ values of 0.026, 0.021 and 0.24 nM for mMAGL, hMAGL and rMAGL, respectively. MAGL-IN-13 can penetrant blood brain barrier. .

HY-147939

AChE/BuChE-IN-3	Cholinesterase (ChE) Amyloid-β	Cancer
AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC₅₀s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ_1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease .

HY-17355S2

Pramipexole-d7-1 dihydrochloride	Dopamine Receptor	Neurological Disease
Pramipexole-d₇-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].

HY-15010

L-371,257	Oxytocin Receptor Vasopressin Receptor	Endocrinology
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (K_i=19 nM) and vasopressin V1a receptor (K_i=3.7 nM) .

HY-109968A

Irdabisant hydrochloride CEP-26401 hydrochloride	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .

HY-109968

Irdabisant CEP-26401	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .

HY-147319

RTI-7470-44	Others	Neurological Disease
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .

HY-144790

AChE-IN-12	Amyloid-β Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC₅₀s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC₅₀ = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu ²⁺-induced Aβ_1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease .

HY-150700

RLX-33	ERK	Metabolic Disease
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC₅₀ values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .

HY-107731

SF 11

Neuropeptide Y Receptor Neurological Disease

SF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist (IC₅₀=199 nM). Antidepressant-like activity .

SF 11	Neuropeptide Y Receptor	Neurological Disease
SF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist (IC₅₀=199 nM). Antidepressant-like activity .

CNS-Penetrant Compound Library	856 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 856 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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-17387

(-)-Huperzine A 3 Publications Verification Huperzine A	Structural Classification Neurological Disease Classification of Application Fields Anti-aging Huperziaceae Source classification Pyridine Alkaloids Plants Alkaloids Terpenoids Sesquiterpenes Huperzia serrata Disease Research Fields	Cholinesterase (ChE) Apoptosis iGluR
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC₅₀ of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .

Cat. No.	Product Name	Chemical Structure

HY-17355S

Pramipexole-d7 dihydrochloride
Pramipexole-d₇ (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

Pramipexole-d7 dihydrochloride

Pramipexole-d₇ (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

HY-17355S1

Pramipexole-d5 dihydrochloride
Pramipexole-d₅ (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

Pramipexole-d5 dihydrochloride

Pramipexole-d₅ (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].

HY-B0410S1

Pramipexole-d5
Pramipexole-d₅ is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].

HY-17355S2

Pramipexole-d7-1 dihydrochloride
Pramipexole-d₇-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].

Pramipexole-d7-1 dihydrochloride

Pramipexole-d₇-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].

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