Istradefylline(KW-6002) (Synonyms: KW 6002) |
| Katalog-Nr.GC11590 |
Istradefyllin (KW-6002) ist ein sehr potenter, selektiver und oral aktiver Adenosin-A2A-Rezeptorantagonist mit einer Ki von 2,2 nM in experimentellen Modellen der Parkinson-Krankheit.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 155270-99-8
Sample solution is provided at 25 µL, 10mM.
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KW-6002 is a selective adenosine A2A receptor antagonist, offering a novel mechanistic approach for the treatment of Parkinson’s disease (PD). A2A blockade will increase in GABAergic inhibition on the medium-sized neurons, leading to a net decrease in excessive activation of striatopallidal output.
In vitro: The affinity of KW-6002 for the A2AR is 70-fold greater than that for the A1 receptor. The binding affinities (Ki) of KW-6002 for human A1 receptor and A2A receptor are >287 nM and 9.12 nM, respectively [1].
In vivo: In MPTP neurotoxin model of PD in mice, KW-6002 significantly attenuated striatal dopamine depletion under various conditions. In addition, pretreatment with KW-6002 (3.3 mg/kg, i.p.) before a single dose of MPTP attenuated the partial dopamine and DOPAC depletions 1 week later [2].
Clinical trial: In a clinical study, the authors evaluated the safety and efficacy of KW-6002 40 mg as monotherapy for Parkinson’s disease (PD) in 176 patients. The primary efficacy outcome was changed from baseline to endpoint, while safe and well-tolerated, failed to show a significant improvement from placebo for this endpoint [1].
References:
[1] Park A, Stacy M. Istradefylline for the treatment of Parkinson's disease. Expert Opin Pharmacother. 2012 Jan;13(1):111-4.
[2] Chen JF, Xu K, Petzer JP, Staal R, Xu YH, Beilstein M, Sonsalla PK, Castagnoli K, Castagnoli N Jr, Schwarzschild MA. Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci. 2001;21(10):RC143.
| Binding experiment [1]: | |
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Binding assays |
Competition analysis of [3H]-ZM241385 and [3H]-DPCPX binding to caudate-putamen membranes from male Lister hooded rats. [3H]-ZM241385 and [3H]-DPCPX binding at 0.3–0.5 nM were assessed in the presence of 1 U/ml adenosine deaminase in a final assay volume of 0.25 ml. |
| Animal experiment [1]: | |
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Animal models |
Lister hooded rats |
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Dosage form |
4 mg/kg KW6002 by intraperitoneal administration |
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Application |
KW6002 has a role for tonic activation of A 2A adenosine receptors in reward-related phenomena. KW6002 increased dopamine overflow in the rat nucleus accumbens, and also elicited place preference and increased locomotor activity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Harper LK, Beckett SR, Marsden CA, McCreary AC, Alexander SP. Effects of the A 2A adenosine receptor antagonist KW6002 in the nucleus accumbens in vitro and in vivo. Pharmacol Biochem Behav. 2006 Jan;83(1):114-21. | |
| Cas No. | 155270-99-8 | SDF | |
| Überlieferungen | KW 6002 | ||
| Chemical Name | 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione | ||
| Canonical SMILES | CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)C=CC3=CC(=C(C=C3)OC)OC)C | ||
| Formula | C20H24N4O4 | M.Wt | 384.43 |
| Löslichkeit | ≥ 8.8mg/mL in DMSO with gentle warming | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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