40 Results for "

peripheral site

" in MedChemExpress (MCE) Product Catalog:
Products (40)

40 Results for "peripheral site" in MCE Product Catalog:

  • Targets Recommended:
3
3 Cited Publications
Cat. No.: HY-101176
CAS No.: 93515-00-5
Purity:  ≥99.0%
Target:  

Melatonin Receptor

Research Areas:  

Cancer

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
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Cat. No.: HY-107322
CAS No.: 104757-53-1
Purity:  99.96%
Synonyms: Mepirodipine hydrochloride; YM-09730-5
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
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Cat. No.: HY-107322A
CAS No.: 104713-75-9
Synonyms: Mepirodipine; YM-09730-5 Free base
Target:  

Calcium Channel

Research Areas:  

Cardiovascular Disease

Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
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Cat. No.: HY-126031
CAS No.: 2055172-60-4
Target:  

DAGL

Research Areas:  

Inflammation/Immunology

(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
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Cat. No.: HY-P1220A
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
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Cat. No.: HY-107322S
CAS No.: 2930289-02-2
Purity:  ≥98.0%
Synonyms: Mepirodipine-d5 hydrochloride; YM-09730-5-d5 hydrochloride
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors .Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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Cat. No.: HY-107322AS1
CAS No.: 2771469-19-1
Purity:  98.97%
Synonyms: Mepirodipine-d5; YM-09730-5-d5 Free base
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
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Cat. No.: HY-N1151
CAS No.: 147517-06-4
Thunberginol C is an orally active, selective, and non-competitive inhibitor of AChE and BChE, with IC50 values of 41.96 and 42.36 μM, respectively. Thunberginol C exerts cytoprotective, pro-collagen type I restorative, MMP-1 inhibitory, hyaluronic acid restorative, anti-photoaging effects in skin cells. Thunberginol C exerts neuroprotective, anxiolytic, TNF-α inhibitory, neuroinflammation inhibitory, and oxidative stress inhibitory effects. Thunberginol C can be used for the research of Alzheimer’s disease, UVB-induced skin photoaging, allergic reactions, oral bacterial infections, and stress-induced anxiety .
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Cat. No.: HY-119292
CAS No.: 553681-56-4
Research Areas:  

Neurological Disease

AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor with Ki values for human AChE (HuAChE) and butyrylcholinesterase (BuChE) of 21.7 and 48.9 μM respectively. AP2238 blocks the pro-fibrotic interaction between the peripheral site of AChE and , and can inhibit Aβ aggregation. AP2238 can be used for the research of Alzheimer's disease .
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Cat. No.: HY-P1220
CAS No.: 526224-73-7
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
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Cat. No.: HY-N8693
CAS No.: 362472-81-9
Withanoside IV is an orally active, blood-brain barrier-permeable withanolide derivative. Withanoside IV specifically binds to the Sudlow I site of HSA, induces secondary structural changes in HSA, and forms stable HSA complexes. Withanoside IV inhibits the enzymatic activity of COX-2. Withanoside IV induces axonal regeneration, peripheral nervous system myelination and increased axonal density in spinal cord tissue, reduces reactive gliosis-related changes, and improves hindlimb motor function. Withanoside IV binds to amyloid-β 1-42 to inhibit its aggregation, induces neurite outgrowth and synapse reconstruction, repairs damaged axons and dendrites, enhances mitochondrial biogenesis, exerts neuroprotective effects via the BDNF and SIRT1 signaling pathways, reduces ROS production and neuronal apoptosis, and ameliorates memory deficits. Withanoside IV inhibits the activity of the SARS-CoV-2 main protease. Withanoside IV can be used in research related to spinal cord injury, Alzheimer's disease, and coronavirus disease 2019 (COVID-19) .
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Cat. No.: HY-149484
Target:  

Cholinesterase (ChE)

Research Areas:  

Neurological Disease

AChE/BChE-IN-15 (Compound 6d) is an AChE/BChE inhibitor, with IC50s of 20 nM and 220 nM respectively. AChE/BChE-IN-15 binds to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active sites of AChE and BChE. AChE/BChE-IN-15 can be used for research of Alzheimer’s disease .
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Cat. No.: HY-W165085
CAS No.: 6266-40-6
Synonyms: Decamethylenebispyridinium dibromide
Target:  

Cholinesterase (ChE)

Research Areas:  

Neurological Disease

1,10-Bis(pyridinium)decane (Decamethylenebispyridinium dibromide) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 25.8 nM. 1,10-Bis(pyridinium)decane acts as a bis-quaternary ligand that bridges the enzyme's catalytic site and peripheral site via its two pyridinium groups. 1,10-Bis(pyridinium)decane can be used for the research of alzheimer's disease .
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Cat. No.: HY-157527
CAS No.: 2978613-03-3
Research Areas:  

Neurological Disease

hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
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Cat. No.: HY-150728
CAS No.: 3032264-62-0
Target:  

Cholinesterase (ChE)

Research Areas:  

Neurological Disease

AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .
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Cat. No.: HY-151885
Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research .
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Cat. No.: HY-163746
Target:  

Cholinesterase (ChE)

Research Areas:  

Neurological Disease

BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
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Cat. No.: HY-120622
CAS No.: 225521-80-2
Target:  

Src

Research Areas:  

Cancer

BMS-243117 is a potent, and selective benzothiazole based p56 Lck inhibitor with an IC50 of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC50 of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck .
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Cat. No.: HY-101176R
CAS No.: 93515-00-5
Research Areas:  

Cancer

2-Iodomelatonin (Standard) is the analytical standard of 2-Iodomelatonin. This product is intended for research and analytical applications. 2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 ?over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
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Cat. No.: HY-129931
CAS No.: 15893-46-6
Synonyms: H-Phe-Phe-NH2
Target:  

Neurokinin Receptor

Research Areas:  

Neurological Disease

Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases .
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