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Results for "

CNS penetrability

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AAK1 (2) Amyloid-β (1) Calcium Channel (2) Cannabinoid Receptor (1) CCR (1) EGFR (1) Eukaryotic Initiation Factor (eIF) (1) GABA Receptor (1) GSK-3 (1) HBV (4) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (1) HIV (5) Influenza Virus (2) Isotope-Labeled Compounds (1) LPL Receptor (2) mAChR (1) mGluR (1) Microtubule/Tubulin (1) nAChR (1) P2X Receptor (1) PARP (1) Reverse Transcriptase (4) Tyrosinase (1)
By Research Areas:	Cancer (8) Endocrinology (1) Infection (7) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (22)

By Targets:

AAK1 (2)

Amyloid-β (1)

Calcium Channel (2)

Cannabinoid Receptor (1)

CCR (1)

EGFR (1)

Eukaryotic Initiation Factor (eIF) (1)

GABA Receptor (1)

GSK-3 (1)

HBV (4)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (1)

HIV (5)

Influenza Virus (2)

Isotope-Labeled Compounds (1)

LPL Receptor (2)

mAChR (1)

mGluR (1)

Microtubule/Tubulin (1)

nAChR (1)

P2X Receptor (1)

PARP (1)

Reverse Transcriptase (4)

Tyrosinase (1)

By Research Areas:

Cancer (8)

Endocrinology (1)

Infection (7)

Inflammation/Immunology (2)

Metabolic Disease (1)

Neurological Disease (22)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-110191

VU0469650	mGluR	Neurological Disease Cancer
VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM .

HY-101281

VU 6008667	mAChR	Neurological Disease
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-164307

Pebezertinib BLU 451; LNG-451	EGFR	Cancer
Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .

HY-B0250

Lamivudine Maximum Cited Publications 6 Publications Verification BCH-189	HIV Reverse Transcriptase HBV	Infection Cancer
Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .

HY-147639

Cav 2.2/3.2 blocker 1	Calcium Channel	Neurological Disease
Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC₅₀ values of 78 μM and 80 μM against Ca_v2.2 and Ca_v3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS .

HY-156986

ITH15004	P2X Receptor	Neurological Disease
ITH15004 is a CNS-penetrated P2X7 antagonist, used for the study of neurodegenerative diseases .

HY-15050

KCL-440	PARP	Neurological Disease Inflammation/Immunology
KCL-440 is a CNS-penetrated PARP inhibitor, with an IC₅₀ of 68 nM. KCL-440 has strong inhibition of PARP-1 .

HY-106578

Quinupramine LM 208	Others	Neurological Disease
Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].

HY-162722

GSK-3 inhibitor 6	GSK-3	Others
GSK-3 inhibitor 6 (2) is a CNS penetrated GSK-3 inhibitor, with IC₅₀ values of 29 nM and 24 nM for GSK-3α and GSK-3β, respectively .

HY-147821

CB1-IN-2	Cannabinoid Receptor	Metabolic Disease
CB1-IN-2 (Compound 4g) is a selective CB₁ inhibitor with an IC₅₀ of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .

HY-119274

BN-82451 dihydrochloride	Others	Neurological Disease
BN-82451 dihydrochloride, an orally active and CNS-penetrated antioxidant and a multitargeting neuroprotective agent, exert a significant protection in experimental animal models mimicking aspects of cerebral ischemia, Parkinson disease, Huntington disease, and more particularly amyotrophic lateral sclerosis .

HY-B0250A

Lamivudine salicylate BCH-189 salicylate	HIV Reverse Transcriptase HBV	Infection Cancer
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .

HY-B0250R

Lamivudine (Standard) BCH-189 (Standard)	HIV Reverse Transcriptase HBV	Infection Cancer
Lamivudine (Standard) is the analytical standard of Lamivudine. This product is intended for research and analytical applications. Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .

HY-17377

Vicriviroc maleate SCH-417690 maleate; SCH-D maleate	CCR HIV	Infection Endocrinology Cancer
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a K_i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC₉₀s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU?570).

HY-114724

HSR-609	Histamine Receptor	Inflammation/Immunology
HSR-609 is an orally active amphoteric antiallergic agent. HSR-609 has a high affinity for histamine H1-receptor in the guinea pig cerebral cortex. HSR-609 inhibits allergic airway hyperresponsiveness to Acetylcholine. HSR-609 shows poor ability to penetrate into the CNS in mice and guinea pigs .

HY-145838

AAK1-IN-4	AAK1	Neurological Disease
AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC₅₀ of 4.6 nM, Filt K_i of 0.9 nM, and cell IC₅₀ of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain .

HY-145839

AAK1-IN-5	AAK1	Neurological Disease
AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC₅₀ of 1.2 nM, Filt K_i of 0.05 nM, and cell IC₅₀ of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain .

HY-B0250S

Lamivudine-15N,d2 BCH-189-¹⁵N,d₂	HBV HIV Reverse Transcriptase Isotope-Labeled Compounds	Infection Cancer
Lamivudine- ¹⁵N,d₂ is ¹⁵N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .

HY-B1080

Tilorone dihydrochloride 2 Publications Verification	HIF/HIF Prolyl-Hydroxylase Influenza Virus	Infection Neurological Disease
Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC₅₀ of 230 nM against Ebola virus (EBOV) .

HY-125021

2BAct 1 Publications Verification	Eukaryotic Initiation Factor (eIF)	Neurological Disease
2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC₅₀ of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .

HY-105066

Davunetide 1 Publications Verification	Microtubule/Tubulin Amyloid-β	Neurological Disease
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .

HY-10035

TTA-P2 2 Publications Verification T-Type calcium channel inhibitor	Calcium Channel	Neurological Disease
TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .

HY-161846

Tyrosinase-IN-31	Tyrosinase	Neurological Disease
Tyrosinase-IN-31 (compound 2-06) is a central-targeting tyrosinase inhibitor (tyrosinase: monophenolase IC₅₀=70.44 μM, diphenolase IC₅₀=1.89 μM). Tyrosinase-IN-31 can inhibit the tyrosinase and melanogenesis. Tyrosinase-IN-31 can penetrate the BBB and enter the central nervous system (CNS). Tyrosinase-IN-31 shows neuroprotective effects and Parkinsonism behavior improving function .

HY-B1080R

Tilorone dihydrochloride (Standard)	HIF/HIF Prolyl-Hydroxylase Influenza Virus	Infection Neurological Disease
Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC₅₀ of 230 nM against Ebola virus (EBOV) .

HY-10035A

(R)-TTA-P2	Others	Neurological Disease
(R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .

HY-50707

(Rac)-TTA-P2 (Rac)-T-Type calcium channel inhibitor	Others	Neurological Disease
(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .

HY-10968A

CYM5442 hydrochloride	LPL Receptor	Neurological Disease
CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC₅₀ of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS) .

HY-10968

CYM5442 1 Publications Verification	LPL Receptor	Neurological Disease
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC₅₀ of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .

HY-138879B

CP-601932 (1S,5R)-CP-601927	nAChR	Neurological Disease
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (K_i=21 nM; EC₅₀=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (K_i=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .

HY-100370

MRK-016	GABA Receptor	Cancer
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77?and 1.4?nM for human?GABA_A?α1β3γ2, GABA_A?α2β3γ2, GABA_A?α3β3γ2, and GABA_A?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

Cat. No.	Product Name

HY-L0124V

Chemspace CNS-Focused Library	13,082 compounds
The basic requirements for the compounds that are supposed to penetrate the blood-brain barrier are somewhat different from those for the majority of drug discovery projects. Alongside the known problem with delivery of the large and non-polar compounds and their penetrability through the cell membrane, the other issue arises as well: small and polar compounds are not able to pass the Blood-Brain Barrier. Chemspace CNS-focused library comprises quite small, non-polar compounds that are also free from PAINS/toxic fragments and aggregators.

Chemspace CNS-Focused Library

13,082 compounds

The basic requirements for the compounds that are supposed to penetrate the blood-brain barrier are somewhat different from those for the majority of drug discovery projects. Alongside the known problem with delivery of the large and non-polar compounds and their penetrability through the cell membrane, the other issue arises as well: small and polar compounds are not able to pass the Blood-Brain Barrier. Chemspace CNS-focused library comprises quite small, non-polar compounds that are also free from PAINS/toxic fragments and aggregators.

Cat. No.	Product Name	Target	Research Area

HY-105066

Davunetide 1 Publications Verification	Microtubule/Tubulin Amyloid-β	Neurological Disease
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .

HY-P2342

Angiopep-Bim BH3 hydrochloride	Peptides	Neurological Disease
Angiopep-Bim BH3 hydrochloride, a BBB penetrated peptode, could be used to investigate the permeability of CNS therapeutics .

HY-P4708

Excitin 1	Peptides	Neurological Disease
Excitin 1 is an orally active and CNS-penetrated peptide, alters behavior and brain monoamine and amino acid concentrations in rats .

Cat. No.	Product Name	Chemical Structure

HY-B0250S

Lamivudine-15N,d2
Lamivudine- ¹⁵N,d₂ is ¹⁵N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .

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