Shopping Cart
- Remove All
Your shopping cart is currently empty
AVN-101
AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
Catalog No. T26690Cas No. 1061354-48-0
Select Batch
Purity:99.73%
Contact us for more batch information
AVN-101
Catalog No. T26690Cas No. 1061354-48-0
AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. 
Product information is being updated, if you want to purchase, please click the bulk custom button.
Bulk & Custom
Questions
View MoreInhibitors Related to "AVN-101"
Famotidine
MK-208
T162776824-35-6
Famotidine (MK-208) is a propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors on the basolateral membrane of parietal cells, famotidine reduces basal and nocturnal gastric acid secretion, thereby decreasing gastric volume, acidity, and the amount of gastric acid released in response to various stimuli.
- $50
Size
QTY
Alverine citrate
NSC 35459
T04285560-59-8
Alverine citrate (NSC 35459) is utilized in functional gastrointestinal disorders.
- $41
Size
QTY
Dapoxetine hydrochloride
Priligy, LY-210448 hydrochloride, LY-210448, Dapoxetine HCl
T6461129938-20-1
Dapoxetine hydrochloride (LY-210448 hydrochloride) is a selectivity short-acting serotonin reuptake inhibitor, used for the therapy of premature ejaculation.
- $30
Size
QTY
Sodium butanoate
Sodium Butyrate, Butanoic acid sodium salt
T1393156-54-7
Sodium butanoate (Sodium Butyrate) is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).
- $33
Size
QTY
Alginic acid
Snow acid algin G, Sazzio, Protanal LF, Norgine, Kelacid
T205979005-32-7
Alginic acid (Snow acid algin G) is a natural polysaccharide extracted from brown seaweeds with anti-anaphylactic and anti-inflammatory activities. Alginic acid inhibits histamine release and can be used in the food industry.
- $29
Size
QTY
Meclizine dihydrochloride
NSC28728, Meclozine dihydrochloride, Meclizine 2HCl
T11101104-22-9
Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.
- $50
Size
QTY
Lidocaine
Xylocaine, Lignocaine, Alphacaine
T0468137-58-6
Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.
- $45
Size
QTY
Octopamine hydrochloride
(±)-p-Octopamine hydrochlorid, (+,-)-Octopamine HCl
T0469770-05-8
Octopamine hydrochloride ((±)-p-Octopamine hydrochlorid) is a biogenic monoamine structurally associated with noradrenaline. It can serve as a neurohormone, a neurotransmitter, and a neuromodulator in invertebrates.
- $45
Size
QTY
Trazodone hydrochloride
Trazodone HCl, KB-831, AF-1161
T161925332-39-2
Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.
- $39
Size
QTY
CLOZAPINE N-OXIDE
Cited
T449434233-69-7
Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.
- $30
Size
QTY
CitedMianserin hydrochloride
ORG GB-94 HCl, Org GB 94, Mianserin HCl
T078321535-47-7
Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant properties that blocks alpha-adrenergic, histamine H1, and certain serotonin receptors; it may cause drowsiness and hematological issues.
- $30
Size
QTY
Dexmedetomidine hydrochloride
Precedex, Dexmedetomidine HCl, (S)-Medetomidine hydrochloride, (+)-Medetomidine hydrochloride
T6466145108-58-3
Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.
- $35
Size
QTY
Product Introduction
Bioactivity
Chemical Properties
| Description | AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases. |
| Targets&IC50 | 5-HT7:153 pM(Ki), α2:0.41-3.6 nM(Ki), H1:0.58 nM(Ki) |
| In vitro | METHODS: The ability of AVN-101 to block hERG channels was tested in single-cell patch clamp experiments using HEK cells stably expressing hERG potassium channels and measuring potassium currents. RESULTS Both AVN-101 and M1 blocked hERG channels with an IC50 score of 0.58 μM. [2] |
| In vivo | METHODS: AVN-101 (5 mg/kg) was evaluated in Wistar rats when administered by oral (PO) and intravenous (I.v) routes. AVN-101 was detected in plasma using LC-MS/MS. RESULTS The bioavailability of AVN-101 in rats (calculated based on AUC0 ⟶240 values) was 26.3% when injected intraperitoneally and 8.5% when administered orally. However, it should be noted that the drug elimination rate determined in the in vivo experiments, Kel = 0.0121 min-1 (i.v.), was significantly slower than that observed in rat microsomes (Kel = 0.335 min-1). [1] |
| Molecular Weight | 340.89 |
| Formula | C21H25ClN2 |
| Cas No. | 1061354-48-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/ml (176.01 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy AVN-101 | purchase AVN-101 | AVN-101 cost | order AVN-101 | AVN-101 chemical structure | AVN-101 in vivo | AVN-101 in vitro | AVN-101 formula | AVN-101 molecular weight
- TOP
Feedback
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.