Istradefylline-13C-d3 (Synonyms: KW-6002-13C,d3) |
| رقم الكتالوجGC47472 |
A neuropeptide with diverse biological activities
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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Istradefylline-13C-d3 is intended for use as an internal standard for the quantification of istradefylline by GC- or LC-MS. Istradefylline is an adenosine receptor 2A (A2A) antagonist (Ki = 2.2 nM in a radioligand binding assay).1 In vivo, istradefylline inhibits catalepsy induced by haloperidol with an ED50 value of 0.23 mg/kg in rats. Oral administration of istradefylline alleviates postural defects in a dose-dependent manner without inducing dyskinesias or hyperactivity in an MPTP-induced marmoset model of Parkinson's disease.2 It also decreases bradykinesias induced by L-DOPA and improves attentional and working memory deficits in an MPTP-induced macaque model of Parkinson's disease.3 Formulations containing istradefylline are used to extend on-time in Parkinson's disease patients experiencing motor fluctuations.
1.Shimada, J., Nobuaki, K., Nonaka, H., et al.Adenosine A2A antagonists with potent anti-cataleptic activityBioorg. Med. Chem. Lett.7(18)2349-2352(1997) 2.Kanda, T., Jackson, M.J., Smith, L.A., et al.Adenosine A2A antagonist: A novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeysAnn. Neurol.43(4)507-513(1998) 3.Ko, W.K.D., Camus, S.M., Li, Q., et al.An evaluation of istradefylline treatment on Parkinsonian motor and cognitive deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaque modelsNeuropharmacology100(Pt. A)48-58(2016)
| Cas No. | N/A | SDF | |
| المرادفات | KW-6002-13C,d3 | ||
| Canonical SMILES | CCN(C(N1CC)=O)C2=C(N([13C]([2H])([2H])[2H])C(/C=C/C3=CC=C(OC)C(OC)=C3)=N2)C1=O | ||
| Formula | C19[13C]H21D3N4O4 | M.Wt | 388.5 |
| الذوبان | DMSO: soluble,Methanol: soluble | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.574 mL | 12.87 mL | 25.74 mL |
| 5 mM | 0.5148 mL | 2.574 mL | 5.148 mL |
| 10 mM | 0.2574 mL | 1.287 mL | 2.574 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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