Search Result

Results for "

CNS penetrant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (1) Angiotensin Receptor (1) Autophagy (3) Beta-secretase (2) Dopamine Receptor (1) Eukaryotic Initiation Factor (eIF) (1) FAAH (1) GCGR (3) GHSR (1) GSK-3 (2) HDAC (2) Interleukin Related (1) IRAK (1) LRRK2 (2) mAChR (3) MAGL (1) MAP3K (1) MARCKS (2) mGluR (7) mTOR (2) Neurokinin Receptor (1) NOD-like Receptor (NLR) (1) Opioid Receptor (1) P-glycoprotein (1) P2X Receptor (4) p38 MAPK (5) Phosphodiesterase (PDE) (2) PI3K (2) ROCK (1) ROR (1) Serotonin Transporter (1) Sodium Channel (1) Somatostatin Receptor (2) Thyroid Hormone Receptor (1) TRP Channel (2) Vasopressin Receptor (1) γ-secretase (2)
By Research Areas:	Cancer (5) Endocrinology (2) Infection (1) Inflammation/Immunology (7) Metabolic Disease (6) Neurological Disease (45)

By Targets:

Anaplastic lymphoma kinase (ALK) (1)

Angiotensin Receptor (1)

Autophagy (3)

Beta-secretase (2)

Dopamine Receptor (1)

Eukaryotic Initiation Factor (eIF) (1)

FAAH (1)

GCGR (3)

GHSR (1)

GSK-3 (2)

HDAC (2)

Interleukin Related (1)

IRAK (1)

LRRK2 (2)

mAChR (3)

MAGL (1)

MAP3K (1)

MARCKS (2)

mGluR (7)

mTOR (2)

Neurokinin Receptor (1)

NOD-like Receptor (NLR) (1)

Opioid Receptor (1)

P-glycoprotein (1)

P2X Receptor (4)

p38 MAPK (5)

Phosphodiesterase (PDE) (2)

PI3K (2)

ROCK (1)

ROR (1)

Serotonin Transporter (1)

Sodium Channel (1)

Somatostatin Receptor (2)

Thyroid Hormone Receptor (1)

TRP Channel (2)

Vasopressin Receptor (1)

γ-secretase (2)

By Research Areas:

Cancer (5)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (7)

Metabolic Disease (6)

Neurological Disease (45)

Inhibitors & Agonists

Screening Libraries

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122138

VU6010572	mGluR	Neurological Disease
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

HY-133554

ASK1-IN-1	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) .

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-12776

GSK805 3 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 .

HY-115726

FRM-024	γ-secretase	Neurological Disease
FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.

HY-117632

Elcubragistat 1 Publications Verification ABX-1431	MAGL	Neurological Disease
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC₅₀ of 14 nM.

HY-114403

VU6012962	mGluR	Neurological Disease
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu₇ NAM) with an IC₅₀ of 347 nM .

HY-118098

LY3202626	Beta-secretase	Neurological Disease
LY3202626 is a CNS penetrant BACE inhibitor with IC₅₀s of 0.615 nM and 0.871 nM against BACE1 and BACE2, respectively .

HY-154958

mTOR inhibitor-12	mTOR	Neurological Disease
mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases .

HY-10869

OL-135	FAAH	Metabolic Disease
OL-135 is a CNS penetrant, selective, and reversible of FAAH inhibitor. OL-135 exhibits analgesic activity .

HY-168025

VU6007496	Others	Neurological Disease
VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .

HY-115726A

(-)-FRM-024	γ-secretase	Neurological Disease
(-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimer’s disease research .

HY-109055

Elenbecestat E2609	Beta-secretase	Neurological Disease
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research .

HY-137061

AZ-GHS-22	GHSR	Metabolic Disease
AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC₅₀=0.77 nM) .

HY-162359

BIO-7488	IRAK	Neurological Disease Inflammation/Immunology
BIO-7488 is a potent, selective, oral active and CNS-penetrant IRAK4 inhibitor with the IC₅₀ of 0.6 nM and > 30 μM for IRAK4 and hERG, respectively .

HY-112286

PI3Kγ inhibitor 2	PI3K	Inflammation/Immunology
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a K_i of 4 nM .

HY-160207

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

HY-107982

VU6005649	mGluR	Neurological Disease
VU6005649 is a CNS penetrant mGlu_7/8 receptor agonist with EC₅₀s of 0.65 μM and 2.6 μM for mGlu₇ receptor and mGlu₈ receptor, respectively.

HY-124382

AS1928370	TRP Channel	Neurological Disease
AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research .

HY-108710

VU0650786 1 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 .

HY-119943

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 .

HY-123481

JNJ-42253432	P2X Receptor	Metabolic Disease
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK_i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively .

HY-120796

MW108 hydrochloride MW01-11-108SRM hydrochloride	p38 MAPK	Neurological Disease
MW108 (MW01-11-108SRM) hydrochloride is a selective and CNS-penetrant p38αMAPK inhibitor with a K_i of 114 nM. MW108 hydrochloride ameliorates beta-amyloid induced synaptic and cognitive dysfunction .

HY-132981

Lu AF27139	P2X Receptor	Neurological Disease
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC₅₀s of 12 and 2.4 nM for human and rat, K_is of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .

HY-100483

A-804598 3 Publications Verification	P2X Receptor	Cancer
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC₅₀s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively .

HY-144372

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 .

HY-116819

VU0453379	GCGR	Metabolic Disease
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC₅₀ of 1.3 μM .

HY-101116

GLP-1R Antagonist 1 2 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 .

HY-116819A

VU0453379 hydrochloride	GCGR	Metabolic Disease
VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC₅₀ of 1.3 μM .

HY-156681

STX-478	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 .

HY-120004

PF-06827443	mAChR	Infection
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .

HY-145778

AGI-41998	Somatostatin Receptor	Neurological Disease
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .

HY-152107

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 .

HY-113616

VU0364572	mAChR MARCKS	Neurological Disease
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor with an EC₅₀ of 0.11 μM. VU0364572 has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 is orally active and is CNS penetrant .

HY-145777

AGI-43192	Somatostatin Receptor	Neurological Disease Cancer
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .

HY-150640

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

HY-150503

KH-259	HDAC	Neurological Disease
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC₅₀ of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .

HY-113616A

VU0364572 TFA	MARCKS mAChR	Neurological Disease
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC₅₀ of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .

HY-121313

Embusartan BAY 10-6734	Angiotensin Receptor	Neurological Disease Endocrinology
Embusartan (BAY 10-6734) is a brain-penetrant and effective AT1 receptor blocker. Embusartan inhibits Ang II binding to brain AT1 receptors in the nuclei of central nervous system (CNS) inside due to high lipophilic character. Embusartan is promising for research of sympathetic hyperactivity and hypertension .

HY-120111

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 .

HY-139279

Zotizalkib 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 .

HY-122647

Valiglurax VU0652957; VU2957	mGluR	Neurological Disease
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC₅₀ values of 64.6 nM and 197 nM for hmGlu₄/Gqi5 and rmGlu₄ GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .

HY-107128

Ampreloxetine hydrochloride TD-9855 hydrochloride	Serotonin Transporter	Neurological Disease
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC₅₀ values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .

HY-14418

VU0361737 ML-128	mGluR	Neurological Disease
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR₄ PAM), with EC₅₀s of 240 nM and 110 nM for human and rat mGluR₄ receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research .

HY-154957

mTOR inhibitor-11	mTOR	Neurological Disease
mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC₅₀: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC₅₀s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease .

HY-128772

XPC-6444	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 .

HY-120111A

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

HY-152107A

(R,R)-LRRK2-IN-7	LRRK2	Neurological Disease
(R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). 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.

HY-120111B

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

HY-123934

VU6007477	P-glycoprotein	Neurological Disease
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC₅₀ value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .

Cat. No.	Product Name

HY-L028

CNS-Penetrant Compound Library

901 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 901 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

446 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 446 approved food additives which are safe substances and can be used for drug discovery and other research.

HY-L061

Orally Active Compound Library

3,774 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 3,774 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.

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

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: