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ALX-420-030 Revised 12-Dec-06
BAY 41-2272
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SYNONYMS 3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY Guanylyl Cyclases, Guanosine Phosphate Metabolism/Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-420-030-M005   5 mg 92.00 USD Add To Cart
ALX-420-030-M025   25 mg 358.00 USD Add To Cart
Product Specification
FORMULA: C20H17FN6
MW: 360.4
PURITY: ≥98%
APPEARANCE: White to off-white needles.
SOLUBILITY: Soluble in DMSO, dichloromethane, 100% ethanol or 2-pyrrolidone. Practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
NO-independent activator of soluble guanylyl cyclase (sGC) [1,2]. Activates both isoforms α1β1 and α1β2 of sGC [3]. While the related compound YC-1 (Prod. No. ALX-420-025) also acts as a non-specific phosphodiesterase inhibitor, BAY 41-2272 has no effect on phosphodiesterases. Stimulation of sGC is not blocked by high concentrations of NO scavengers (e.g. PTIO, Prod. No. ALX-430-007) and the combination of  BAY 41-2272 with the NO donor DEA NONOate (Prod. No. ALX-430-034) potentiates the activation of sGC. Although BAY 41-2272 alone is not as strong a stimulator of sGC as NO, concentrations as low as 10-100nM stimulate sGC to a level that would be expected to cause biologically important increases in cGMP [1]. ODQ (Prod. No. ALX-270-034), a potent and selective inhibitor of sGC, completely inhibited the effect of BAY 41-2272 [1]. The activity of BAY 41-2272 is described in selected literature references [4-6].
Product Specific Literature References
[1] NO-independent regulatory site on soluble guanylate cyclase: J.P. Stasch, et al.; Nature 410, 212 (2001) Abstract
[2] NO-independent regulatory site of direct sGC stimulators like YC-1 and BAY 41-2272: E.M. Becker, et al.; BMC Pharmacol. 1, 13 (2001) Abstract; Full Text
NO-independent stimulators of soluble guanylate cyclase: A. Straub, et al.; Bioorg. Med. Chem. Lett. 11, 781 (2001) Abstract
[3] BAY 41-2272 activates two isoforms of nitric oxide-sensitive guanylyl cyclase: M. Koglin, et al.; BBRC 292, 1057 (2002) Abstract
[4] Cardiorenal and humoral properties of a novel direct soluble guanylate cyclase stimulator BAY 41-2272 in experimental congestive heart failure: G. Boerrigter, et al.; Circulation 107, 686 (2003) Abstract
[5] BAY 41-2272: a stimulator of soluble guanylyl cyclase induces nitric oxide-dependent penile erection in vivo: E. Bischoff, et al.; Urology 61, 464 (2003) Abstract
[6] Macrophage endothelial nitric oxide synthase auto-regulates cellular activation and pro-inflammatory protein expression: L. Connelly, et al.; J. Biol. Chem 278, 26480 (2003) Abstract; Full Text
Antiinflammatory activity of soluble guanylate cyclase: cGMP-dependent down-regulation of P-selectin expression and leukocyte recruitment: A. Ahluwalia, et al.; PNAS 101, 1386 (2004) Abstract; Full Text
Identification of residues crucially involved in soluble guanylate cyclase activation: C. Rothkegel, et al.; FEBS Lett. 580, 4205 (2006) Abstract
 
 
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