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Results for "

brain-penetrable

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Amyloid-β (1) Autophagy (2) Bacterial (3) Beta-secretase (1) Cannabinoid Receptor (3) Caspase (1) CRFR (2) Dopamine Receptor (6) EGFR (2) Histamine Receptor (2) Indoleamine 2,3-Dioxygenase (IDO) (3) Isotope-Labeled Compounds (1) LRRK2 (2) MCHR1 (GPR24) (1) mGluR (1) MNK (1) nAChR (1) Neurokinin Receptor (1) NO Synthase (1) Opioid Receptor (1) Oxytocin Receptor (1) Phosphodiesterase (PDE) (1) Phospholipase (1) Reference Standards (3) Ribosomal S6 Kinase (RSK) (2) UGT (1) γ-secretase (1)
By Research Areas:	Cancer (12) Endocrinology (4) Infection (4) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (19)

By Targets:

5-HT Receptor (2)

Amyloid-β (1)

Autophagy (2)

Bacterial (3)

Beta-secretase (1)

Cannabinoid Receptor (3)

Caspase (1)

CRFR (2)

Dopamine Receptor (6)

EGFR (2)

Histamine Receptor (2)

Indoleamine 2,3-Dioxygenase (IDO) (3)

Isotope-Labeled Compounds (1)

LRRK2 (2)

MCHR1 (GPR24) (1)

mGluR (1)

MNK (1)

nAChR (1)

Neurokinin Receptor (1)

NO Synthase (1)

Opioid Receptor (1)

Oxytocin Receptor (1)

Phosphodiesterase (PDE) (1)

Phospholipase (1)

Reference Standards (3)

Ribosomal S6 Kinase (RSK) (2)

UGT (1)

γ-secretase (1)

By Research Areas:

Cancer (12)

Endocrinology (4)

Infection (4)

Inflammation/Immunology (3)

Metabolic Disease (5)

Neurological Disease (19)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10510

BI-D1870 Maximum Cited Publications 18 Publications Verification	Ribosomal S6 Kinase (RSK) Autophagy	Cancer
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .

HY-14136

Rimonabant 10+ Cited Publications SR141716	Cannabinoid Receptor Bacterial	Infection Metabolic Disease Cancer
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a K_i of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-111540

LY-3381916 2 Publications Verification IDO1-IN-5	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
LY-3381916 (IDO1-IN-5) is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .

HY-120789

PF-06648671	γ-secretase	Neurological Disease
PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease .

HY-120085

PFE-360 3 Publications Verification PF-06685360	LRRK2	Neurological Disease
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC₅₀ of 2.3 nM in vivo .

HY-131703

UGT8-IN-1 1 Publications Verification	UGT	Metabolic Disease
UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders .

HY-14130

CP 376395	CRFR	Neurological Disease Endocrinology
CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist .

HY-13488

HG-10-102-01 1 Publications Verification	LRRK2 MNK	Neurological Disease
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC₅₀ values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC₅₀ values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research .

HY-124322

NB-360	Beta-secretase Amyloid-β	Neurological Disease Inflammation/Immunology
NB-360 is a potent, brain penetrable and orally active β‐secretase 1/2 (BACE1/BACE2) dual inhibitor with IC₅₀ values of 5 and 6 nM. NB-360 can inhibit amyloid-β protein accumulation. NB-360 can be used for the researches of inflammation and neurological disease, such as Alzheimer's disease .

HY-106000

GSK239512	Histamine Receptor	Neurological Disease
GSK239512 is a potent and brain penetrated H₃ receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD) .

HY-10847B

SB-277011 hydrochloride 1 Publications Verification SB-277011A hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor (D₃R) antagonist with K_i values of 10.7 nM and 11.2 nM at rodent and human D₃R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK_is of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT_1B, and 5-HT_1D receptors, respectively .

HY-136146

SUVN-911	nAChR	Neurological Disease
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K_i of 1.5 nM. SUVN-911 has antidepressant activity .

HY-N4134

Ciwujianoside C3	NO Synthase	Inflammation/Immunology
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .

HY-107691

GR 159897	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK₂) receptor antagonist. GR 159897 has little or no affinity for NK₁ and NK₃ receptors. GR 159897 inhibits binding of [ ³H]GR100679 to human NK₂ (hNK₂)-CHO cells and rat colon membranes with pK_is of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .

HY-116941

A-381393	Dopamine Receptor	Neurological Disease
A-381393 is a potent, selective, brain penetrate dopamine D₄ receptor antagonist, with K_is of 1.5, 1.9 and 1.6 nM for human dopamine D_4.4, D_4.2, and D_4.7 receptor, respectively, >2700-fold selectivity over D₁, D₂, D₃ and D₅ dopamine receptors. A-381393 shows moderate affinity for 5-HT_2A (K_i, 370 nM) .

HY-128351

SHR1653 1 Publications Verification	Oxytocin Receptor	Neurological Disease Endocrinology
SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC₅₀ of 15 nM for hOTR .

HY-101188

INCB38579	Histamine Receptor	Infection
INCB38579 is an orally active, highly brain penetrable, and selective histamine H₄ receptor (HH₄R) antagonist (hH₄R IC₅₀=4.8 nM, mH₄R IC₅₀=42 nM, rH₄R IC₅₀=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .

HY-12697

NGB 2904	Dopamine Receptor	Neurological Disease
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .

HY-111540B

(S)-LY-3381916 1 Publications Verification (S)-IDO1-IN-5	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
(S)-LY-3381916 ((S)-IDO1-IN-5; Example 1B) is an active S-isomer of LY-3381916. (S)-LY-3381916 binds to IDOL with an IC₅₀ value less than 1.5 µΜ . LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .

HY-136208

TAN-452	Opioid Receptor	Neurological Disease
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a K_i of 0.47 nM and a K_b of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; K_i=36.56 nM and K_b=9.43 nM) and κ-opioid receptor (KOR; K_i=5.31 nM and K_b=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .

HY-131204

CZL80	Caspase	Neurological Disease
CZL80, a brain-penetrable caspase-1 inhibitor with an IC₅₀ of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility .

HY-100605

VU0483605	mGluR	Others
VU0483605 is a potent and brain-penetrated mGlu₁ receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu₁ PAM activity at both human and rat, with EC₅₀ values of 390 and 356 nM, respectively .

HY-14136S

Rimonabant-d10 SR141716-d₁₀	Isotope-Labeled Compounds Cannabinoid Receptor Bacterial	Infection Metabolic Disease Cancer
Rimonabant-d₁₀ is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-153856

TAS2940	EGFR	Cancer
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC₅₀ values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .

HY-103379

CP 376395 hydrochloride	CRFR	Neurological Disease Endocrinology
CP 376395 hydrochloride is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist .

HY-107623

TC-MCH 7c	MCHR1 (GPR24)	Metabolic Disease
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH₁R antagonist with an IC₅₀ of 5.6 nM for hMCH₁R . TC-MCH 7c has K_is of 3.4 nM and 3.0 nM of human and mouse MCH₁R, respectively .

HY-149025

DPTIP-prodrug 18 P18	Phospholipase	Inflammation/Immunology Cancer
DPTIP-proagent 18 (P18) is a orally active and brain-penetrable proagent of DPTIP (HY-131002). DPTIP-proagent 18 is a potent nSMase2 inhibitor. DPTIP-proagent 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-proagent 18 can be used for brain injury research .

HY-153856A

TAS2940 fumarate	EGFR	Cancer
TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC₅₀ values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .

HY-128349

MT-3014	Phosphodiesterase (PDE)	Neurological Disease
MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC₅₀s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively .

HY-14136R

Rimonabant (Standard) SR141716 (Standard)	Cannabinoid Receptor Bacterial Reference Standards	Infection Metabolic Disease Cancer
Rimonabant (Standard) is the analytical standard of Rimonabant. This product is intended for research and analytical applications. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-10847A

SB-277011 dihydrochloride SB-277011A dihydrochloride	Dopamine Receptor	Neurological Disease
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor antagonist, with pK_is of 8.0, 6.0, <5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1D receptors, respectively.

HY-111540A

(Rac)-LY-3381916 (Rac)-IDO1-IN-5	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
(Rac)-LY-3381916 ((Rac)-IDO1-IN-5; Example 1) is a racemate of LY-3381916 . LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .

HY-12697A

NGB 2904 hydrochloride	Dopamine Receptor	Neurological Disease
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .

HY-10510R

BI-D1870 (Standard)	Autophagy Ribosomal S6 Kinase (RSK) Reference Standards	Cancer
BI-D1870 (Standard) is the analytical standard of BI-D1870 (HY-10510). This product is intended for research and analytical applications. BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .

HY-10847BR

SB-277011 hydrochloride (Standard) SB-277011A hydrochloride (Standard)	Reference Standards Dopamine Receptor 5-HT Receptor	Neurological Disease
SB-277011 hydrochloride (Standard) is the analytical standard of SB-277011 (hydrochloride) (HY-10847B). This product is intended for research and analytical applications. SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with K_i values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK_is of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N4134

Ciwujianoside C3	Structural Classification Acanthopanax henryi (Oliv.) Harms Classification of Application Fields Terpenoids Plants Pentacyclic Triterpenoids Inflammation/Immunology Disease Research Fields Araliaceae Source Classification	NO Synthase
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .

Cat. No.	Product Name	Chemical Structure

HY-14136S

Rimonabant-d10
Rimonabant-d₁₀ is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

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