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CNS-penetration

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenylate Cyclase (1) Anaplastic lymphoma kinase (ALK) (4) Apoptosis (1) Dopamine Receptor (2) Drug Metabolite (2) DYRK (2) EGFR (1) Glucosylceramide Synthase (GCS) (1) Isotope-Labeled Compounds (1) mAChR (1) MAP3K (1) mGluR (1) Microtubule/Tubulin (1) Parasite (1) Prostaglandin Receptor (1) Proteasome (2) Raf (1) Sodium Channel (1) TRP Channel (1)
By Research Areas:	Cancer (7) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (15)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-130121

MK-8719

Others Neurological Disease

MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (K_i=7.9 nM for hOGA) with excellent CNS penetration .

MK-8719	Others	Neurological Disease
MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (K_i=7.9 nM for hOGA) with excellent CNS penetration .

HY-16617

Auglurant VU0424238	mGluR	Neurological Disease
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC₅₀ value of 11 nM (rat) and an IC₅₀ value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration .

HY-101789

Nav1.7-IN-3	Sodium Channel	Neurological Disease
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC₅₀ of 8 nM. Pain relief. Limited CNS penetration .

HY-101281

VU 6008667

VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .

VU 6008667
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .

HY-111258

GSK345931A	Prostaglandin Receptor	Neurological Disease Inflammation/Immunology
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .

HY-17595

Mebendazole 3 Publications Verification	Parasite Apoptosis Microtubule/Tubulin	Infection Cancer
Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .

HY-116016

Etilevodopa L-DOPA ethyl ester; Levodopa ethyl ester	Dopamine Receptor Drug Metabolite	Neurological Disease
Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .

HY-116016A

Etilevodopa hydrochloride L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride	Dopamine Receptor Drug Metabolite	Neurological Disease
Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .

HY-163131

Glucosylceramide synthase-IN-4	Glucosylceramide Synthase (GCS)	Neurological Disease
Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC₅₀ of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity .

HY-145086

R-PSOP	Others	Metabolic Disease
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the K_is of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .

HY-109189

Rezivertinib BPI-7711	EGFR	Cancer
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .

HY-144695

Dyrk1A/α-synuclein-IN-1	DYRK	Neurological Disease
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC₅₀ values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .

HY-144696

Dyrk1A/α-synuclein-IN-2	DYRK	Neurological Disease
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC₅₀ of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .

HY-13011

Alectinib Maximum Cited Publications 26 Publications Verification CH5424802; RO5424802; RG7853	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .

HY-108460

A-784168	TRP Channel	Neurological Disease
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .

HY-114331

DLK-IN-1	MAP3K	Neurological Disease
DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a K_i of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.

HY-147405

Tinlorafenib PF-07284890; ARRY-461	Raf	Cancer
Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC₅₀s of 4.25 and 2.7 nM for BRAF ^V600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies .

HY-13011A

Alectinib Hydrochloride Maximum Cited Publications 26 Publications Verification CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC₅₀ of 1.9 nM and a K_d value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC₅₀s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .

HY-13011S

Alectinib-d8 CH5424802-d₈; RO5424802-d₈; AF802-d₈	Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₈ is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

HY-13011S1

Alectinib-d6 CH5424802-d₆; RO5424802-d₆; AF802-d₆	Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK)	Cancer
Alectinib-d₆ is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

HY-120184

VU0467485 AZ13713945	mAChR	Neurological Disease
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC₅₀s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .

HY-145830

AC1-IN-1	Adenylate Cyclase	Neurological Disease
AC1-IN-1 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC₅₀ of 0.54 µM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity .

HY-109001

Alicapistat 1 Publications Verification ABT-957	Proteasome	Neurological Disease
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC₅₀ value of 395 nM .

HY-109001A

(1S,2R)-Alicapistat (1S,2R)-ABT-957	Proteasome	Neurological Disease
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC₅₀ value of 395 nM .

Alectinib-d8
Alectinib-d₈ is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

Alectinib-d6
Alectinib-d₆ is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

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