AT 1015 |
| رقم الكتالوجGC16807 |
Long-acting 5-HT2A antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 190508-50-0
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');)
;)
AT 1015 is a potent antagonist of 5-HT2A receptor [1].
The 5-HT2A receptor is a G protein-coupled receptor and a subtype of the 5-HT2 receptor, which belongs to the serotonin receptor family. The 5-HT2A receptor plays an important role in clathrin mediated endocytosis of JC virus, the human polyoma virus which causes progressive multifocal leukoencephalopathy (PML).
AT 1015 is a potent 5-HT2A receptor antagonist. AT 1015 bound to 5-HT2 receptors in rabbit cerebral cortex membrane with pKi value of 7.94 [1].
In a photochemically induced rat femoral arterial thrombosis (PIT) model, AT 1015 (1 mg/kg) significantly inhibited vascular contraction induced by 5-HT and prolonged the time for 24 h that required to occlusion of the artery in a dose-dependent way. While, AT 1015 (10 mg/kg) didn’t prolong bleeding time in the tail transection bleeding time test [2]. AT 1015 inhibited 5-HT2A receptor-mediated platelet aggregation both in vitro and in rat. In the rat peripheral vascular lesion model, AT 1015 (1 mg/kg) significantly inhibited progression of peripheral vascular lesions [3].
References:
[1]. Rashid M, Watanabe M, Nakazawa M, et al. Assessment of affinity and dissociation ability of a newly synthesized 5-HT2 antagonist, AT-1015: comparison with other 5-HT2 antagonists. Jpn J Pharmacol, 2001, 87(3): 189-194.
[2]. Kihara H, Koganei H, Hirose K, et al. Antithrombotic activity of AT-1015, a potent 5-HT(2A) receptor antagonist, in rat arterial thrombosis model and its effect on bleeding time. Eur J Pharmacol, 2001, 433(2-3): 157-162.
[3]. Kihara H, Hirose K, Koganei H, et al. AT-1015, a novel serotonin (5-HT)2 receptor antagonist, blocks vascular and platelet 5-HT2A receptors and prevents the laurate-induced peripheral vascular lesion in rats. J Cardiovasc Pharmacol, 2000, 35(4): 523-530.
| Cas No. | 190508-50-0 | SDF | |
| Chemical Name | (Z)-N-(2-(4-(5H-dibenzo[a,d][7]annulen-5-ylidene)piperidin-1-yl)ethyl)-1-formylpiperidine-4-carbimidic acid hydrochloride | ||
| Canonical SMILES | O=CN1CCC(/C(O)=N/CCN2CC/C(CC2)=C3C4=CC=CC=C4C=CC5=CC=CC=C5\3)CC1.Cl | ||
| Formula | C29H33N3O2.HCl | M.Wt | 492.05 |
| الذوبان | <49.2mg/ml in Water; <49.2mg/ml in DMSO | 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 | 2.0323 mL | 10.1616 mL | 20.3231 mL |
| 5 mM | 0.4065 mL | 2.0323 mL | 4.0646 mL |
| 10 mM | 0.2032 mL | 1.0162 mL | 2.0323 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 9 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 *