A 844606 |
| Catalog No.GC15333 |
α7 nAChR partial agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 861119-08-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
A 844606 is a potent and selective partial agonist of α7 nicotinic acetylcholine receptor (nAChR) with IC50 value of 11 nM [1].
The α7 nAChR is a nicotinic acetylcholine receptor and is located in the brain, spleen and lymphocytes of lymph nodes. The α7 nAChR plays an important role in the pathophysiology of neuropsychiatric diseases such as Alzheimer’s disease, schizophrenia, drug addiction and depression [2].
A 844606 is a potent and selective α7 nAChR partial agonist with IC50 values of 11 and >30000 nM for α7 and α4β2, respectively. In Xenopus oocytes expressed recombinant human and rat α7 nAChR, A 844606 showed agonist activity with EC50 values of 1.4 and 2.2 μM, respectively. In PC12 cells, A 844606 activated α7 nAChR, which stimulated ERK1/2 phosphorylation [1].
In the mouse brain, A 844606 showed high uptake. In monkey brain, A 844606 was mainly distributed in the thalamus and hippocampus and was low in the cerebellum. Also, A 844606 was reduced by pretreatment with SSR180711, an α7 nAChR agonist [2].
References:
[1]. Briggs CA, Schrimpf MR, Anderson DJ, et al. alpha7 nicotinic acetylcholine receptor agonist properties of tilorone and related tricyclic analogues. Br J Pharmacol, 2008, 153(5): 1054-1061.
[2]. Toyohara J, Ishiwata K, Sakata M, et al. In vivo evaluation of alpha7 nicotinic acetylcholine receptor agonists [11C]A-582941 and [11C]A-844606 in mice and conscious monkeys. PLoS One, 2010, 5(2): e8961.
| Cas No. | 861119-08-6 | SDF | |
| Chemical Name | 2-((3aR,6aR)-5-methylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-9H-xanthen-9-one | ||
| Canonical SMILES | O=C1C2=CC(N3C[C@@H](CN(C)C4)[C@H]4C3)=CC=C2OC5=CC=CC=C15 | ||
| Formula | C20H20N2O2 | M.Wt | 320.38 |
| Solubility | <1.6mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1213 mL | 15.6065 mL | 31.2129 mL |
| 5 mM | 0.6243 mL | 3.1213 mL | 6.2426 mL |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1213 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *