Search Result

Results for "

BBB penetrant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amyloid-β (2) Cholinesterase (ChE) (3) DNA/RNA Synthesis (2) Dopamine Receptor (9) EGFR (1) Endogenous Metabolite (1) ERK (1) Estrogen Receptor/ERR (5) GPR52 (1) Histamine Receptor (3) Isotope-Labeled Compounds (3) Monoamine Oxidase (2) nAChR (1) Neurokinin Receptor (1) Opioid Receptor (6) Phosphodiesterase (PDE) (1) Raf (1) Reactive Oxygen Species (1) Sigma Receptor (2) Thymidylate Synthase (1) Topoisomerase (1)
By Research Areas:	Cancer (12) Endocrinology (1) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (26)

By Targets:

Amyloid-β (2)

Cholinesterase (ChE) (3)

DNA/RNA Synthesis (2)

Dopamine Receptor (9)

EGFR (1)

Endogenous Metabolite (1)

ERK (1)

Estrogen Receptor/ERR (5)

GPR52 (1)

Histamine Receptor (3)

Isotope-Labeled Compounds (3)

Monoamine Oxidase (2)

nAChR (1)

Neurokinin Receptor (1)

Opioid Receptor (6)

Phosphodiesterase (PDE) (1)

Raf (1)

Reactive Oxygen Species (1)

Sigma Receptor (2)

Thymidylate Synthase (1)

Topoisomerase (1)

By Research Areas:

Cancer (12)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (1)

Metabolic Disease (1)

Neurological Disease (26)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-15722

SB-222200 3 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-136430

JCN037 JGK037	EGFR	Cancer
JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC₅₀ values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively .

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-117501

Dexchlorpheniramine	Histamine Receptor	Inflammation/Immunology Cancer
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-120946

VMY-2-95	nAChR	Neurological Disease
VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .

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-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-P1335

CTAP	Opioid Receptor	Neurological Disease
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

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-102050

PF-05085727	Phosphodiesterase (PDE)	Neurological Disease
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC₅₀=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .

HY-P1335A

CTAP TFA 1 Publications Verification	Opioid Receptor	Neurological Disease
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

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-A0031

Bazedoxifene Maximum Cited Publications 12 Publications Verification TSE-424	Estrogen Receptor/ERR	Cancer
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

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-A0031A

Bazedoxifene hydrochloride TSE-424 hydrochloride	Estrogen Receptor/ERR	Cancer
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .

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 5 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 5 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 5 Publications Verification	Dopamine Receptor	Neurological Disease
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-12153

JNJ-1930942	Cholinesterase (ChE)	Neurological Disease
JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca ²⁺ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .

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-A0031S

Bazedoxifene-d4 TSE-424-d₄	Isotope-Labeled Compounds Estrogen Receptor/ERR	Cancer
Bazedoxifene-d₄ is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].

HY-A0031R

Bazedoxifene (Standard)	Estrogen Receptor/ERR	Cancer
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .

HY-A0031S2

Bazedoxifene-d4 acetate TSE-424-d₄ acetate	Estrogen Receptor/ERR	Cancer
Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].

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-B0410R

Pramipexole (Standard)	Dopamine Receptor	Neurological Disease
Pramipexole (Standard) is the analytical standard of Pramipexole. This product is intended for research and analytical applications. 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-B0410AR

Pramipexole dihydrochloride hydrate (Standard)	Dopamine Receptor	Neurological Disease
Pramipexole (dihydrochloride hydrate) (Standard) is the analytical standard of Pramipexole (dihydrochloride hydrate). This product is intended for research and analytical applications. Pramipexole dihydrochloride hydrate 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 hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .

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-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-D0186R

2'-Deoxyuridine (Standard)	Endogenous Metabolite Thymidylate Synthase	Infection
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 .

Cat. No.	Product Name

HY-L028

*CNS-Penetrant* Compound Library**	877 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 877 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.

CNS-Penetrant Compound Library

877 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 877 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	Target	Research Area

HY-P1335A

CTAP TFA 1 Publications Verification	Opioid Receptor	Neurological Disease
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

HY-P1335

CTAP	Opioid Receptor	Neurological Disease
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-D0186R

2'-Deoxyuridine (Standard)	Structural Classification Natural Products Immune System Disorder Microorganisms Source classification Disease markers Endogenous metabolite	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 .

Cat. No.	Product Name	Chemical Structure

HY-A0031S

Bazedoxifene-d4

Bazedoxifene-d₄ is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].

HY-A0031S2

Bazedoxifene-d4 acetate

Bazedoxifene-d₄ (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].

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].

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].

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].

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks