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brain+penetration

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) ADC Payload (1) Adrenergic Receptor (1) Amyloid-β (2) Calcium Channel (2) Cannabinoid Receptor (1) Cholinesterase (ChE) (2) Cytochrome P450 (2) Dopamine Receptor (4) EGFR (1) Epigenetic Reader Domain (1) Fungal (1) HDAC (1) Histamine Receptor (4) iGluR (1) Isotope-Labeled Compounds (3) mAChR (1) mGluR (1) Monoamine Transporter (1) Myosin (1) nAChR (2) NO Synthase (1) Opioid Receptor (1) Orexin Receptor (OX Receptor) (2) PARP (2) Phosphodiesterase (PDE) (1) PI3K (1) Potassium Channel (2) Prolyl Endopeptidase (PREP) (1) Reference Standards (1) Sigma Receptor (1) Sodium Channel (2) Src (1) Tau Protein (2) TGF-β Receptor (1) Topoisomerase (1) α-synuclein (1)
By Research Areas:	Cancer (9) Endocrinology (1) Infection (2) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (25)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16712

LDN-214117 2 Publications Verification	TGF-β Receptor	Cancer
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC₅₀ value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC₅₀ value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .

HY-175188

MT-110 BPN-0027490	Myosin	Neurological Disease
MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder .

HY-127106

VU0810464 1 Publications Verification	Potassium Channel	Neurological Disease
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC₅₀=165 nM) and GIRK1/4 (EC₅₀=720 nM) channels with improved brain penetration .

HY-12844

Ro 64-6198 1 Publications Verification	Opioid Receptor	Neurological Disease
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC₅₀ value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .

HY-116578

Metopimazine 3 Publications Verification EXP999; RP9965	Dopamine Receptor	Neurological Disease
Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .

HY-164782

PT3	HDAC	Neurological Disease Metabolic Disease Cancer
PT3 is a selective inhibitor of HDAC3 with an IC₅₀ value of 0.25 μM. PT3 exhibits good brain penetration ability and bioavailability upon oral administration. PT3 can be used in the research of Alzheimer’s disease .

HY-108340

PF-06767832	mAChR	Neurological Disease
PF-06767832 is a potent muscarinic M1 selective positive allosteric modulator (PAM), with the EC₅₀ of 60 nM. PF-06767832 has good brain penetration .

HY-101834

ACT-462206	Orexin Receptor (OX Receptor)	Others
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .

HY-145313

TTBK1-IN-2	Tau Protein	Neurological Disease
TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC₅₀s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice .

HY-120124

Samelisant SUVN-G3031	Histamine Receptor	Neurological Disease
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; K_i=8.7 nM) and rat (rH3R;K_i=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .

HY-148825

NP10679	iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor	Metabolic Disease Inflammation/Immunology Cancer
NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC₅₀s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC₅₀s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes .

HY-167876

PQR514	PI3K	Cancer
PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .

HY-W278021

BTA-1	Amyloid-β	Others
BTA-1 is an uncharged derivative of thioflavin-T. BTA-1 has a high affinity for Aβ fibrils and shows very good brain penetration and clearance .

HY-155672

JPC0323	5-HT Receptor	Neurological Disease
JPC0323 is a dual 5-HT_2C/5-HT_2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .

HY-139300A

Epitinib succinate HMPL-813 succinate	EGFR	Cancer
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) 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-167927

Mefuparib CVL218	PARP	Cancer
Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.

HY-120574

TH1338	ADC Payload Topoisomerase	Cancer
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .

HY-11045

PF-03654746	Histamine Receptor	Neurological Disease Inflammation/Immunology Endocrinology
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis . PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .

HY-15112

JTP-4819	Prolyl Endopeptidase (PREP)	Infection
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC₅₀s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096) .

HY-115727

BET-IN-1	Epigenetic Reader Domain	Others
BET-IN-1 is a potent BET inhibitor that has excellent brain penetration and reasonable metabolic stability.

HY-122787

Tylocrebrine	Others	Others
Tylocrebrine is a compound with anticancer activity. Its clinical research was interrupted due to toxicity issues. By making it into targeted nanoparticles, its inhibitory index can be improved, the killing effect on tumor cells can be enhanced and brain penetration can be reduced.

HY-152632

BuChE-IN-7	Cholinesterase (ChE)	Neurological Disease
BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC₅₀ values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things .

HY-171195

VU0631019	5-HT Receptor	Metabolic Disease
VU0631019 is a potent antagonist of 5-HT_2B, with the IC₅₀ of 29 nM. VU0631019 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .

HY-10030

Mardepodect succinate PF-2545920 succinate	Phosphodiesterase (PDE)	Neurological Disease
Mardepodect succinate (PF-2545920 succinate) is a potent and specific phosphodiesterase 10A (PDE10A) inhibitor with potential activity in the treatment of schizophrenia. Mardepodect succinate has been further optimized to improve brain penetration and compound-like properties for use in schizophrenia research .

HY-171194

VU0530244	5-HT Receptor	Metabolic Disease
VU0530244 is a potent antagonist of 5-HT_2B, with the IC₅₀ of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans .

HY-107666

PHA 568487	nAChR	Neurological Disease Inflammation/Immunology
PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR) .PHA 568487 reduces neuroinflammation and oxidative stress . PHA-568487 has rapid brain penetration .

HY-161380

Antifungal agent 96	Fungal	Infection
Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .

HY-167927S

Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide	Isotope-Labeled Compounds PARP	Cancer
Mycophenolic Acid-d₃ Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.

HY-138879

CP-601927	nAChR	Neurological Disease
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (K_i=1.2 nM; EC₅₀=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .

HY-145906

D4R antagonis-2	Dopamine Receptor	Neurological Disease
D4R antagonist-2 is a potent and selective D4R antagonist with an IC₅₀ of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .

HY-149065

D-685	α-synuclein	Neurological Disease
D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .

HY-158627

JPC0323 Oleate	5-HT Receptor	Others
JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT_2C/5-HT_2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .

HY-174381

BChE-IN-41	Cholinesterase (ChE) Amyloid-β Tau Protein	Neurological Disease
BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC₅₀ =12 nM, K_i= 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ_1-42 .

HY-152171

GZ-11608	Monoamine Transporter	Neurological Disease
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .

HY-135478

LY393615 NCC1048	Calcium Channel Sodium Channel	Neurological Disease
LY393615 (NCC1048) is a novel neuronal Ca ²⁺ (calcium channel) and Na ⁺ channel (sodium channel) blocker with IC₅₀s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research .

HY-155992

WLB-89462	Sigma Receptor	Neurological Disease
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (K_i: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .

HY-135478A

LY393615 free base NCC1048 free base	Calcium Channel Sodium Channel	Neurological Disease
LY393615 (NCC1048) free base is a novel neuronal Ca ²⁺ (calcium channel) and Na ⁺ channel (sodium channel) blocker with IC₅₀s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 free base has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research .

HY-172808

BNS808	Cannabinoid Receptor Cytochrome P450	Metabolic Disease
BNS808 is an orally active and selective cannabinoid-1 receptor (CB₁R) antagonist (IC₅₀ = 0.8 nM) with notable CB₂R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding .

HY-122608

Samelisant free base SUVN-G3031 free base	Histamine Receptor	Neurological Disease
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; K_i=8.7 nM) and rat (rH3R;K_i=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .

HY-143994S

Metopimazine acid-d6 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Metopimazine-d₆ hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .

HY-157998

mG2N001	mGluR Src	Others
mG2N001 is a negative allosteric modulator (NAM) (IC₅₀: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope ^[11C]mG2N001 can be used in PET imaging. ^[11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .

HY-116578S

Metopimazine-d6 EXP999-d₆; RP9965-d₆	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Metopimazine-d₆ (EXP999-d₆; RP9965-d₆) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .

HY-101834R

ACT-462206 (Standard)	Reference Standards Orexin Receptor (OX Receptor)	Others
ACT-462206 (Standard) is the analytical standard of ACT-462206 (HY-101834). This product is intended for research and analytical applications. ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .

HY-181711

nNOS-IN-6	NO Synthase	Neurological Disease Cancer
nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS K_i of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS K_i of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .

Cat. No.	Product Name	Chemical Structure

HY-167927S

Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide
Mycophenolic Acid-d₃ Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.

HY-143994S

Metopimazine acid-d6 hydrochloride

Metopimazine-d₆ hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .

HY-116578S

Metopimazine-d6

Metopimazine-d₆ (EXP999-d₆; RP9965-d₆) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .

Cat. No.	Product Name		Classification

HY-139300A

Epitinib succinate HMPL-813 succinate		Alkynes
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) 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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