Unii-950o97nupo
- Product Name
- Unii-950o97nupo
- CAS No.
- 377727-87-2
- Chemical Name
- Unii-950o97nupo
- Synonyms
- MK3814;CS-672;MK 3814;MK-3814;Preladent;SCH-420814;Preladenant;Unii-950o97nupo;Preladenant (MK-3814;Sch 420814 Preladenant
- CBNumber
- CB82520825
- Molecular Formula
- C25H29N9O3
- Formula Weight
- 503.56
- MOL File
- 377727-87-2.mol
Unii-950o97nupo Property
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H319Causes serious eye irritation
H361Suspected of damaging fertility or the unborn child
H372Causes damage to organs through prolonged or repeated exposure
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P281Use personal protective equipment as required.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P308+P313IF exposed or concerned: Get medical advice/attention.
P314Get medical advice/attention if you feel unwell.
P391Collect spillage. Hazardous to the aquatic environment
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 22210
- Product name
- Preladenant
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $86
- Updated
- 2024/03/01
- Product number
- 22210
- Product name
- Preladenant
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $356
- Updated
- 2024/03/01
- Product number
- 22210
- Product name
- Preladenant
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $629
- Updated
- 2024/03/01
- Product number
- 22210
- Product name
- Preladenant
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $1152
- Updated
- 2024/03/01
- Product number
- P712600
- Product name
- Preladenant
- Packaging
- 50mg
- Price
- $3520
- Updated
- 2021/12/16
Unii-950o97nupo Chemical Properties,Usage,Production
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] ROBERT A HODGSON. Characterization of the potent and highly 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]pyrimidin-5-amine] in rodent models of movement disorders and depression.[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 330 1: 294-303. DOI:10.1124/jpet.108.149617
[2] ROBERT A. HODGSON . Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders[J]. Experimental Neurology, 2010, 225 2: Pages 384-390. DOI:10.1016/j.expneurol.2010.07.011
[3] ANNALISA PINNA PHD, DVM. Antidyskinetic effect of A2A and 5HT1A/1B receptor ligands in two animal models of Parkinson’s disease[J]. Movement Disorders, 2016, 31 4: 501-511. DOI:10.1002/mds.26475
[4] PAUL A BEAVIS. Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2013, 110 36: 14711-14716. DOI:10.1073/pnas.1308209110
[5] STEPHEN M HATFIELD Michail S. A2A adenosine receptor antagonists to weaken the hypoxia-HIF-1α driven immunosuppression and improve immunotherapies of cancer[J]. Current Opinion in Pharmacology, 2016, 29: Pages 90-96. DOI:10.1016/j.coph.2016.06.009
[6] OHTA A. A Metabolic Immune Checkpoint: Adenosine in Tumor Microenvironment.[J]. Frontiers in Immunology, 2016: 109. DOI:10.3389/fimmu.2016.00109
[7] NCT03099161
Unii-950o97nupo Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Unii-950o97nupo manufacturers
- Product
- Preladenant 377727-87-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10
- Product
- Preladenant 377727-87-2
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-08