| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
A-867744 targets the alpha7 nicotinic acetylcholine receptor (α7 nAChR) as a type II positive allosteric modulator. The α7 nAChR is a ligand-gated ion channel involved in cognitive function, sensory gating, and neuroprotection. Unlike orthosteric agonists that bind to the acetylcholine binding site, positive allosteric modulators like A-867744 bind to a separate site on the receptor and enhance the receptor's response to endogenous acetylcholine. A-867744 has also been reported to target the muscarinic acetylcholine receptor M5 (CHRM5) and neuronal acetylcholine receptor beta-2 (CHRNB2).
|
|---|---|
| ln Vitro |
A-867744 potentiates acetylcholine (ACh)-evoked currents at α7 nAChRs with an EC50 of approximately 1.0 μM. In Xenopus laevis oocytes expressing human or rat α7 receptors, A-867744 potentiates ACh-evoked currents with IC50 values of 0.98 μM and 1.12 μM for human and rat α7 receptors, respectively. The compound has been reported to have high purity (>99.7%) and is commonly provided as a 10 mM solution in DMSO for biochemical assays. It is a type II PAM with good potency and selectivity.
|
| ln Vivo |
A-867744 has demonstrated acceptable pharmacokinetic properties across multiple species and achieves sufficient levels in the brain to modulate α7 nAChRs. In rodent models of sensory gating, A-867744 has shown efficacy in modulating α7 nAChR-mediated responses. The compound's in vivo activity supports its utility as a research tool for studying the role of α7 nAChRs in cognitive function and neuropsychiatric disorders. Detailed in vivo efficacy data from specific animal models are limited in publicly available sources.
|
| Enzyme Assay |
In non-cell-based receptor binding and functional assays, A-867744's activity at the α7 nAChR is evaluated using radioligand binding and electrophysiological techniques. For binding studies, membrane preparations from cells expressing α7 nAChRs are incubated with a radiolabeled α7-selective ligand and varying concentrations of A-867744 to determine its affinity. For functional characterization, the compound's ability to potentiate ACh-evoked currents is measured in Xenopus laevis oocytes injected with α7 nAChR cRNA using two-electrode voltage clamp electrophysiology. These assays have established A-867744's EC50 of approximately 1 μM.
|
| Cell Assay |
In vitro cellular assays for A-867744 involve measuring its effects on α7 nAChR-mediated calcium flux or electrophysiological responses in cultured cells. Cell lines expressing recombinant α7 nAChRs are treated with A-867744 in the presence of a sub-maximal concentration of acetylcholine, and receptor activation is assessed by measuring changes in intracellular calcium using fluorescence-based plate readers (FLIPR assays). The compound's ability to potentiate ACh-evoked responses is quantified to determine its PAM activity and potency. These functional assays have confirmed A-867744's EC50 of approximately 1.0 μM.
|
| Animal Protocol |
In vivo animal studies for A-867744 have been conducted in rodent models to assess its effects on sensory gating and cognitive function. In sensory gating rodent models, A-867744 has been shown to modulate α7 nAChR-mediated responses. The compound is typically administered via oral or intraperitoneal routes, and its brain penetration has been confirmed. Behavioral assays such as prepulse inhibition of startle are used to evaluate sensory gating, while novel object recognition or Morris water maze tests are used to assess cognitive function.
|
| ADME/Pharmacokinetics |
A-867744 has demonstrated acceptable pharmacokinetic properties across multiple species. The compound achieves sufficient levels in the brain to modulate α7 nAChRs. It is available as a 10 mM solution in DMSO and as solid quantities for formulation. The compound's pharmacokinetic profile supports its use in in vivo studies. Specific parameters such as half-life, bioavailability, and clearance have not been extensively reported in publicly available sources but are described as acceptable for research purposes.
|
| Toxicity/Toxicokinetics |
Detailed toxicological data for A-867744 are limited in publicly available sources. As a research compound intended for laboratory use, comprehensive toxicology studies have not been extensively published. The compound is supplied as a high-purity research-grade chemical (>99.7%) and is not intended for human use. Researchers should handle the compound with appropriate safety precautions, including the use of personal protective equipment and proper waste disposal procedures, as is standard for all research chemicals.
|
| Additional Infomation |
A-867744 (compound 19) is a novel type II PAM of the α7 nAChR with good potency and selectivity. It has been investigated for its potential to modulate α7 nAChR function in the context of cognitive disorders and neuropsychiatric conditions. The compound has shown acceptable pharmacokinetics across species and brain penetration sufficient to modulate α7 nAChRs. A-867744 is a research chemical and is not an approved drug. It is available from various research chemical suppliers for laboratory use only.
|
| Molecular Formula |
C20H19CLN2O3S
|
|---|---|
| Molecular Weight |
402.893
|
| Exact Mass |
402.08
|
| CAS # |
1000279-69-5
|
| PubChem CID |
23642319
|
| Appearance |
White to yellow solid powder
|
| LogP |
6.127
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
620
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ABACVOXFUHDKNZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H19ClN2O3S/c1-3-20(24)18-12-19(14-4-6-15(21)7-5-14)23(13(18)2)16-8-10-17(11-9-16)27(22,25)26/h4-12H,3H2,1-2H3,(H2,22,25,26)
|
| Chemical Name |
4-(5-(4-Chlorophenyl)-2-methyl-3-propionylpyrrol-1-yl)benzenesulfonamide
|
| Synonyms |
A 867744 A867744A-867744
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~248.21 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4821 mL | 12.4103 mL | 24.8207 mL | |
| 5 mM | 0.4964 mL | 2.4821 mL | 4.9641 mL | |
| 10 mM | 0.2482 mL | 1.2410 mL | 2.4821 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
