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Submit ReviewKW 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.
KW 3902 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 356.46 |
Formula | C20H28N4O2 |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 136199-02-5 |
PubChem ID | 64627 |
InChI Key | PJBFVWGQFLYWCB-UHFFFAOYSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 17.82 | 50 | |
ethanol | 8.91 | 25 |
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.
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 |
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.
Keywords: KW 3902, KW 3902 supplier, adenosine, a1, antagonists, selective, KW3902, Rolofylline, Adenosine, A1, Receptors, 4167, Tocris Bioscience
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
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Average Rating: 5 (Based on 1 Review.)
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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).