- Preladenant
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- $34.00 / 1mg
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2024-11-19
- CAS:377727-87-2
- Min. Order:
- Purity: 98.18%
- Supply Ability: 10g
- Preladenant
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- $15.00 / 1KG
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2021-07-13
- CAS:377727-87-2
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- Preladenant
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- $15.00 / 1KG
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2021-07-09
- CAS:377727-87-2
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
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| | Unii-950o97nupo Basic information |
| Product Name: | Unii-950o97nupo | | Synonyms: | 2-(2-Furanyl)-7-[2-[4-[4-(2-Methoxyethoxy)phenyl]-1-piperazinyl]ethyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyriMidin-5-aMine;2-Furan-2-yl-7-(2-{4-[4-(2-Methoxy-ethoxy)-phenyl]-piperazin-1-yl}-ethyl)-7,9a-dihydro-5H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyriMidin-5-ylaMine;7H-Pyrazolo(4,3-E)(1,2,4)triazolo(1,5-C)pyrimidin-5-amine, 2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-;Preladenant;SCH-420814;Unii-950o97nupo;2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)-ethyl)-7H-pyrazolo[4,3-e][1,2,4;Sch 420814 Preladenant | | CAS: | 377727-87-2 | | MF: | C25H29N9O3 | | MW: | 503.56 | | EINECS: | | | Product Categories: | Amines;Pharmaceuticals;Intermediates & Fine Chemicals;Heterocycles;Aromatics | | Mol File: | 377727-87-2.mol |  |
| | Unii-950o97nupo Chemical Properties |
| density | 1.47±0.1 g/cm3(Predicted) | | storage temp. | -20° | | solubility | Soluble in DMSO (up to 5 mg/ml with warming). | | form | solid | | pka | 6.42±0.40(Predicted) | | color | Beige | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| | Unii-950o97nupo Usage And Synthesis |
| Description | Preladenant is an orally bioavailable antagonist of the adenosine A2A receptor (Kis = 1.1 and 2.5 nM for human and rat receptors, respectively). It is selective for A2A receptors over A1, A2B, and A3 receptors (Kis = >1,000, >1,700, and >1,000 nM, respectively) as well as a panel of 59 receptors, enzymes, and ion channels. Preladenant inhibits adenylate cyclase activity (Kbs = 1.3 and 0.7 nM for human and rat receptors, respectively) induced by the A2A receptor agonist CGS 21680 . It inhibits catalepsy induced by haloperidol in rats by 77 and 70% after 1 and 4 hours, respectively, when administered at a dose of 1 mg/kg. Preladenant also increases the efficacy of L-DOPA when used in combination with eltoprazine in a 6-OHDA rat lesion model of Parkinson’s disease dyskinesia. | | Uses | A potent and selective antagonist at the adenosine A2A receptor. It is being researched as a potential treatment for Parkinson''s disease. | | in vivo | Preladenant (1 mg/kg) inhibits L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Preladenant exhibits antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test[1]. Preladenant produces a dose-dependent reduction in parkinsonian scores at doses of 1 mg/kg (min score: 9.0) and 3 mg/kg (min score: 6.5). A subthreshold dose of Preladenant reduces minimum and mean parkinsonian scores in animals treated with 3 mg kg of L-Dopa to 5.25 and 6.88 respectively. A Wilcoxin test is used to compare individual treatments against vehicle. Preladenant (3 mg/kg), L-Dopa (3, 6, and 12 mg/kg), and the combination of Preladenant and L-Dopa (1 or 3 mg/kg+3 mg/kg) are all significantly improved on the minimum parkinsonian score. In addition, both the 12 mg/kg L-Dopa and L-Dopa+Preladenant groups are significantly improved on both minimum and mean parkinsonian scores relative to the 3 mg/kg L-Dopa group[2]. | | target | adenosine A2A receptor | | References | 1)?Hodgson?et al.?(2009), Characterization of the potent and selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimodin-5-amine] in rat models of movement disorders and depression;?J.Pharmacol.Exp.Ther.?330294
2)?Hodgson?et al.?(2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders;?Exp.Neurol.?225384
3)?Pinna?et al.?(2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson’s disease;?Mov.Disord.?31501
4)?Beavis?et al.?(2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors;?Proc.Natl.Acad.Sci USA.?11014711
5)?Hatfield and Sitkovsky (2016), A2A adenosine receptor antagonist to weaken the hypoxia-HIF-1a driven immunosuppression and improve immunotherapies of cancer;?Curr.Opin.Pharmacol.?2990
6)?Ohta?et al.?(2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment;?Front.Immunol.?71
7)?NCT03099161 |
| | Unii-950o97nupo Preparation Products And Raw materials |
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