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KW-6356

Cat. No. M25400

All AbMole products are for research use only, cannot be used for human consumption.

KW-6356 Structure

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Quality Control & Documentation
Biological Activity

KW-6356 is a potent and selective adenosine A2A receptor antagonist/inverse agonist and exhibits insurmountable antagonism. KW-6356 is a potent and selective ligand for the A2A receptor (the −log of inhibition constant = 9.93 ± 0.01 for human receptor) with a very low dissociation rate from the receptor (the dissociation kinetic rate constant = 0.016 ± 0.006 /min for human receptor). In particular, in vitro functional studies indicated that KW-6356 exhibits insurmountable antagonism and inverse agonism, while istradefylline exhibits surmountable antagonism.

Chemical Information
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Yutaro Ohno, et al. J Pharmacol Sci. The adenosine A2A receptor antagonist/inverse agonist, KW-6356 enhances the anti-parkinsonian activity of L-DOPA with a low risk of dyskinesia in MPTP-treated common marmosets

[2] Yutaro Ohno, et al. Eur J Pharmacol. Anti-parkinsonian activity of the adenosine A2A receptor antagonist/inverse agonist KW-6356 as monotherapy in MPTP-treated common marmosets

[3] Yutaro Ohno, et al. Mol Pharmacol. In Vitro Pharmacological Profile of KW-6356, a Novel Adenosine A2A Receptor Antagonist/Inverse Agonist

[4] Tomonori Tayama, et al. Clin Pharmacol Drug Dev. Safety, Tolerability, and Pharmacokinetics of the Novel Adenosine A2A Antagonist/Inverse Agonist KW-6356 Following Single and Multiple Oral Administration in Healthy Volunteers

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Istradefylline

Istradefylline (KW-6002) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM.

CGS 21680

CGS 21680 is a selective adenosine receptor agonist for A2A and A3 with Ki of 15 ng/mL and 37 ng/mL, respectively.

Norisoboldine

Norisoboldine is an isoquinoline alkaloid which acts as an AhR agonist.

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Keywords: KW-6356 supplier, Adenosine Receptor, inhibitors, activators

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