© 2008 Alexis Corporation
ALX-420-030
Revised 24-Sep-08
BAY 41-2272
SYNONYMS
3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1
H
-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
ALX-420-030-M025
25 mg
358.00 USD
Product Specification
FORMULA:
C
20
H
17
FN
6
MW:
360.4
CAS NUMBER:
256376-24-6
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
HAZARD:
IRRITANT.
Product Description
NO-independent activator of soluble guanylyl cyclase (sGC) [1,2]. Activates both isoforms α
1
β
1
and α
1
β
2
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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