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Istradefylline - ≥99%, high purity , Adenosine A2a receptor antagonist, CAS No.155270-99-8, Adenosine A2a receptor antagonist

  • Moligand™
  • ≥99%
Item Number
I125338
Grouped product items
SKUSizeAvailabilityPrice Qty
I125338-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$14.90
I125338-25mg
25mg
In stock
$61.90
I125338-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$205.90
I125338-1g
1g
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,854.90

Competitive inhibitor of adenosine A2A receptors

Basic Description

SynonymsIstradefylline|155270-99-8|KW-6002|nouriast|Nourianz|Istradefylline (KW-6002)|KW 6002|8-[(E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione|(E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methyl-1H-purine-2,6(3H,7H)-dione|KW6002|Istradef
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsIstradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist in experimental models of Parkinson's disease. Istradefylline reduces dyskinesia resulting from long-term treatment with classical antiparkinson drugs such
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAdenosine A2a receptor antagonist
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Toxic, refer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.
A selective A(2A) antagonist used to study parkinson’s disease in vitro

Product Properties

ALogP2.5

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD2 Tclin D(2) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH3 Tclin Histamine H3 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PGR Tclin Progesterone receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDE4A Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MC3R Tchem Melanocortin receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA2A Tclin Adenosine receptor A2a 17 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA2B Tclin Adenosine receptor A2b 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRNA4 Tclin Neuronal acetylcholine receptor subunit alpha-4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ACHE Tclin Acetylcholinesterase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA2A Tclin Alpha-2A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRB1 Tclin Beta-1 adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAOB Tclin Amine oxidase [flavin-containing] B 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA1 Tclin Adenosine receptor A1 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR1A Tclin 5-hydroxytryptamine receptor 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TBXA2R Tclin Thromboxane A2 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

F2 Tclin Prothrombin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

OPRM1 Tclin Mu-type opioid receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione
INCHI InChI=1S/C20H24N4O4/c1-6-23-18-17(19(25)24(7-2)20(23)26)22(3)16(21-18)11-9-13-8-10-14(27-4)15(12-13)28-5/h8-12H,6-7H2,1-5H3/b11-9+
InChi Key IQVRBWUUXZMOPW-PKNBQFBNSA-N
Canonical SMILES CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)C=CC3=CC(=C(C=C3)OC)OC)C
Isomeric SMILES CCN1C2=C(C(=O)N(C1=O)CC)N(C(=N2)/C=C/C3=CC(=C(C=C3)OC)OC)C
WGK Germany 3
PubChem CID 5311037
Molecular Weight 384.43

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

3 results found

Lot NumberCertificate TypeDateItem
H1813172Certificate of AnalysisFeb 21, 2024 I125338
H1813171Certificate of AnalysisMay 12, 2022 I125338
E1624040Certificate of AnalysisJan 19, 2022 I125338

Chemical and Physical Properties

SolubilityDMSO 6 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
SensitivityHeat Sensitive
Melt Point(°C)193 °C

Safety and Hazards(GHS)

Pictogram(s) GHS06
Signal Danger
Hazard Statements

H301:Toxic if swallowed

Precautionary Statements

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P301+P316:IF SWALLOWED: Get emergency medical help immediately.

WGK Germany 3

Related Documents

References

1. Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Westerhout J, Spangenberg T, Brussee J, Ijzerman AP.  (2007)  2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists..  J Med Chem,  50  (4): (828-34).  [PMID:17300165]
2. Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE.  (2011)  International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update..  Pharmacol Rev,  63  (1): (1-34).  [PMID:21303899]
3. Dungo R, Deeks ED.  (2013)  Istradefylline: first global approval..  Drugs,  73  (8): (875-82).  [PMID:23700273]

Solution Calculators