Stimulator of soluble guanylate cyclase
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BAY 41-8543

Item No. 10011131

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-4,6-pyrimidinediamine
CAS Number
256498-66-5
Molecular Formula
C21H21FN8O
Formula Weight
420.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/ml
λmax
212, 327 nm
SMILES
FC(C=CC=C1)=C1CN2N=C(C3=NC(N)=C(N4CCOCC4)C(N)=N3)C5=C2N=CC=C5
InChi Code
InChI=1S/C21H21FN8O/c22-15-6-2-1-4-13(15)12-30-21-14(5-3-7-25-21)16(28-30)20-26-18(23)17(19(24)27-20)29-8-10-31-11-9-29/h1-7H,8-12H2,(H4,23,24,26,27)
InChi Key
AQYFUZRYBJBAGZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Soluble guanylate cyclase (sGC) is the primary cellular receptor for nitric oxide (NO). NO binds and activates a heme group in sGC, initiating the conversion of GTP to the second messenger cyclic GMP (cGMP). BAY 41-8543 is a heme-dependent stimulator of sGC, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold.1 Surprisingly, NO donors synergize with BAY 41-8543 in stimulating recombinant sGC.1 BAY 41-8543 relaxes vessels and inhibits platelet aggregation in vitro at nM concentrations.1 In vivo, BAY 41-8543 decreases blood pressure dose-dependently, prolongs bleeding time, and reduces thrombosis.2 Inhalation of microparticles containing BAY 41-8543 increases pulmonary vasodilation without changing mean arterial pressure,3 suggesting that agonists of sGC may be efficacious in treating pulmonary hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stasch, J.-P., Alonso-Alija, C., Apeler, H., et al. Pharmacological actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: In vitro studies. Br. J. Pharmacol. 135(2), 333-343 (2002).

    2. Stasch, J.P., Dembowsky, K., Perzborn, E., et al. Cardiovascular actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: In vivo studies. Br. J. Pharmacol. 135(2), 344-355 (2002).

    3. Evgenov, O.V., Kohane, D.S., Bloch, K.D., et al. Inhaled agonists of soluble guanylate cyclase induce selective pulmonary vasodilation. Am. J. Respir. Crit. Care Med. 176(11), 1138-1145 (2007).