1. GPCR/G Protein
  2. Adenosine Receptor
  3. Istradefylline

Istradefylline  (Synonyms: KW-6002)

Cat. No.: HY-10888 Purity: 99.70%
COA Handling Instructions

Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

For research use only. We do not sell to patients.

Istradefylline Chemical Structure

Istradefylline Chemical Structure

CAS No. : 155270-99-8

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10 mM * 1 mL in DMSO
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10 mg USD 66 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Istradefylline:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

IC50 & Target

Ki: 2.2 nM (adenosine A2A receptor)

In Vitro

Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2 nM versus 150 nM[1]. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes[4]. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat, 105.02 nM and 1.87 nM for A1 receptor and A2A receptor in mouse, respectively[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Istradefylline (3.3 mg/kg, i.p.) treatment before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later[1]. Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with an ED50 of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs. Istradefylline combined with L-dopa cuases potent effects on haloperidol-induced and reserpine-induced catalepsy[2]. Istradefylline (10 mg/kg, p.o.) results an increase in locomotor activity to approximately twice that of control and improves motor disability in MPTP-treated common marmosets. Istradefylline (10 mg/kg, p.o.) in combination with SKF80723, quinpirole, or L-DOPA produces a significant additive effect on locomotor activity and improvement of motor disability but not dysKinesia[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

384.43

Formula

C20H24N4O4

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1C2=C(N=C(/C=C/C3=CC(OC)=C(OC)C=C3)N2C)N(CC)C(N1CC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25.33 mg/mL (65.89 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.70%

References
Cell Assay
[5]

A CHO cell line permanently expressing the human adenosine A1or A2A receptor is cultured in α-MEM supplemented with 10% (v/v) fetal bovine serum, 50 U/mL penicillin, and 50 μg/mL streptomycin. Cells are grown at 37°C in an environment of 5% CO2. These cells are seeded on black 96-well assay plates at a density of 15,000 cells/well, and then they are cultured for 24 h.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

The animals are housed either in pairs or alone under standard conditions at a temperature of 24-26°C and 50-60% relative humidity using a 12-h light-dark cycle. Diet consisted of standard food pellets, fresh fruit, and Mazuri marmoset jelly. The animals are treated with MPTP in a dose of 2.0 mg/kg sc daily for 5 days. Following MPTP treatment the animals are allowed to recover from the acute effects over a period of some 6-8 weeks. During MPTP treatment and throughout the following weeks, the animals are hand-fed with Mazuri marmoset jelly and fresh fruit puree until they are able to maintain them-selves. Prior to behavioral testing, from 6-8 weeks to 8 months after exposure to MPTP, all animals show a marked reduction of basal locomotor activity, slower and less coordinated movements, abnormal postures of some parts of the body, and reduced checKing movements and eye blinks. Istradefylline (KW-6002) is suspended in 0.3% Tween-80 and 10% sucrose solution and administered in a final volume of 2.0 mL/kg body weight by oral gavage.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6013 mL 13.0063 mL 26.0125 mL 65.0313 mL
5 mM 0.5203 mL 2.6013 mL 5.2025 mL 13.0063 mL
10 mM 0.2601 mL 1.3006 mL 2.6013 mL 6.5031 mL
15 mM 0.1734 mL 0.8671 mL 1.7342 mL 4.3354 mL
20 mM 0.1301 mL 0.6503 mL 1.3006 mL 3.2516 mL
25 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
30 mM 0.0867 mL 0.4335 mL 0.8671 mL 2.1677 mL
40 mM 0.0650 mL 0.3252 mL 0.6503 mL 1.6258 mL
50 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3006 mL
60 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0839 mL
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Istradefylline Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Istradefylline
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HY-10888
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