36 Results for "

brain-penetrating

" in MedChemExpress (MCE) Product Catalog:
Products (36)

36 Results for "brain-penetrating" in MCE Product Catalog:

2
2 Cited Publications
Cat. No.: HY-B2132
CAS No.: 61-54-1
Synonyms: 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .
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1
1 Cited Publications
Cat. No.: HY-111791
CAS No.: 1708113-43-2
Purity:  99.80%
Target:  

HDAC

Research Areas:  

Cancer

ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
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1
1 Cited Publications
Cat. No.: HY-109058
CAS No.: 648927-86-0
Purity:  ≥98.0%
Synonyms: QGC001; RB150
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .
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1
1 Cited Publications
Cat. No.: HY-148236
CAS No.: 2741956-55-6
Purity:  99.74%
Target:  

TRP Channel

Research Areas:  

Inflammation/Immunology

BAY-390, a chemical probe, is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .
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Cat. No.: HY-160019
CAS No.: 2750895-97-5
Research Areas:  

Neurological Disease

MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
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Cat. No.: HY-P4073
CAS No.: 1075214-55-9
Synonyms: GRN1005; Paclitaxel trevatide
Research Areas:  

Cancer

ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
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Cat. No.: HY-112723
CAS No.: 1838651-58-3
Purity:  99.83%
Synonyms: ACT-709478
Target:  

Calcium Channel

Research Areas:  

Neurological Disease

Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies .
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Cat. No.: HY-14880
CAS No.: 929622-08-2
Purity:  96.60%
Synonyms: JNJ-31001074
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .
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Cat. No.: HY-111409
CAS No.: 2095515-38-9
Purity:  99.96%
Target:  

RIP kinase

Research Areas:  

Inflammation/Immunology

RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04) .
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Cat. No.: HY-109118A
CAS No.: 1791396-46-7
Purity:  99.62%
Synonyms: SUVN-502 mesylate
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease .
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Cat. No.: HY-107691
CAS No.: 158848-32-9
Purity:  ≥99.0%
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 pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
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Cat. No.: HY-P99530
CAS No.: 1815583-32-4
Synonyms: AGT-181; HIRMAb-IDUA

Target:  

Insulin Receptor

Research Areas:  

Metabolic Disease

Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .
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Cat. No.: HY-12697
CAS No.: 189060-98-8
Purity:  98.28%
Target:  

Dopamine Receptor

Research Areas:  

Neurological Disease

NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
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Cat. No.: HY-14880B
CAS No.: 1103522-80-0
Purity:  99.26%
Synonyms: JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate
Bavisant (JNJ31001074AAC) dihydrochloride hydrate is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .
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Cat. No.: HY-151797
CAS No.: 2368927-41-5
Target:  

CaMK

Research Areas:  

Neurological Disease

Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .
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Cat. No.: HY-100605
CAS No.: 1623101-11-0
Purity:  97.30%
Target:  

mGluR

Research Areas:  

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 .
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Cat. No.: HY-105235
CAS No.: 124378-77-4
Synonyms: CI-977
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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Cat. No.: HY-10623
CAS No.: 862282-10-8
Target:  

Melanocortin Receptor

Research Areas:  

Endocrinology

PF-00446687 hydrochloride is a potent, brain-penetrating, selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 12 nM. PF-00446687 hydrochloride can be used in the research of sexual dysfunction .
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Cat. No.: HY-137440B
CAS No.: 2692692-00-3
Purity:  99.85%
Synonyms: (2R,3R)-TAK-994 free base
Research Areas:  

Neurological Disease

(2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton (HY-137440). Firazorexton is an orally active, brain-penetrating orexin type 2 receptor (OX2R) agonist that may improve narcolepsy-like symptoms ..
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Cat. No.: HY-109118
CAS No.: 701205-60-9
Synonyms: SUVN-502 free base
Target:  

5-HT Receptor

Research Areas:  

Neurological Disease

Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease .
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