KW 3902

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Description: Selective A1 antagonist
Alternative Names: Rolofylline
Chemical Name: 8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione
Purity: ≥99% (HPLC)
Citations (1)
Reviews (1)

Biological Activity for KW 3902

KW 3902 is a selective adenosine A1 receptor antagonist; displays 890-fold selectivity for rat A1 receptors over A2A receptors (Ki values are 0.19 and 170 nM respectively). Displays no effect on recombinant rat A3 receptors expressed on CHO cells at concentrations up to 10 μM. Exhibits diuretic and renal protective effects in rats.

Compound Libraries for KW 3902

KW 3902 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for KW 3902

M. Wt 356.46
Formula C20H28N4O2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 136199-02-5
PubChem ID 64627
Smiles O=C1C2=C(NC(C34CC(CC4C5)CC5C3)=N2)N(CCC)C(N1CCC)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KW 3902

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 17.82 50
ethanol 8.91 25

Preparing Stock Solutions for KW 3902

The following data is based on the product molecular weight 356.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.61 mL 28.05 mL 56.11 mL
2.5 mM 1.12 mL 5.61 mL 11.22 mL
5 mM 0.56 mL 2.81 mL 5.61 mL
25 mM 0.11 mL 0.56 mL 1.12 mL

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References for KW 3902

References are publications that support the biological activity of the product.

Shimada et al (1992) 8-polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors. J.Med.Chem. 35 924 PMID: 1548682

Nonaka et al (1996) KW-3902, a selective high affinity antagonist for adenosine A1 receptors. Br.J.Pharmacol. 117 1645 PMID: 8732272

Nishiyama et al (1999) Adenosine A1 receptor antagonist KW-3902 prevents hypoxia-induced renal vasoconstriction. J.Pharmacol.Exp.Ther. 291 988 PMID: 10565815

If you know of a relevant reference for KW 3902, please let us know.

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Keywords: KW 3902, KW 3902 supplier, adenosine, a1, antagonists, selective, KW3902, Rolofylline, Adenosine, A1, Receptors, 4167, Tocris Bioscience

1 Citation for KW 3902

Citations are publications that use Tocris products. Selected citations for KW 3902 include:

Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806

Do you know of a great paper that uses KW 3902 from Tocris? Please let us know.

Reviews for KW 3902

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systemic administration of KW3902.
By Ariel Vitenzon on 01/05/2018
Assay Type: In Vivo
Species: Mouse

We injected this drug at 1 mg/Kg and 2 mg/Kg systemically (IP) into transgenic mice and monitored the effect on motor behavior. The drug efficiently induced motor symptoms in the transgenic mice at these concentrations.

The drug dissolves well in saline + 0.3% tween 80 with 3X vortex (1min) and sonicate (5min).