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Exclusively from Sigma-RBI
Prod. No. M 6316
Adenosine (Prod. No. A 9251) receptors have been implicated in
the etiology of various cardiovascular, inflammatory and neurological diseases.
Four adenosine receptor subtypes have been identified and are referred to as A1, A2A, A2B and
A3. A2B adenosine receptors stimulate adenylyl cyclase, increase intracellular calcium release and are involved
in the control of vascular tone, cell growth and gene expression, mast cell degranulation and intestinal water
secretion [1].
Sigma-RBI is pleased to introduce MRS 1754, a selective, high-affinity A2B adenosine
receptor antagonist.
- Binds to human A2B and A2A adenosine receptors expressed in
HEK-293 cells with KD values of
1.13 nM and >50 nM, respectively [2].
- Does not bind to membranes expressing rat or human A1 or A3 receptors.
- Displaces both [3H]-ZM 241385 and [125I]-I-ABOPX (non-selective antagonists) from
human A2B adenosine receptors with Ki values of 1.97 nM [2].
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Manufactured and sold under exclusive license from Adenosine Therapeutics, LLC.
References
- Kim, Y-C., et al., J. Med. Chem., 43, 1165-1172 (2000).
- Ji, X-D., et al., Biochem. Pharmacol., 61, 657-663 (2001).
MRS 1754 is featured in Celltransmissions Volume 18, No. 4.
Click here to preview the product highlight.
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