BAY-41-8543 Exclusive

Cayman Chemical Item Number 10011131

(CAS 256498-66-5)

BAY-41-8543 (CAS 256498-66-5)

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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.

1 Stasch, J., 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 135 333-343 (2002).

2 Stasch, J., 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 135 344-355 (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 1138-1145 (2007).

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
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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FC(C=CC=C1)​=C1CN2N=C(C3=NC(N)​=C(N4CCOCC4)​C(N)​=N3)​C5=C2N=CC=C5
InCHI Code
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​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
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AQYFUZRYBJBAGZ-UHFFFAOYSA-N

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Size Price Quantity Subtotal
1 mg $51.00 $0.00
5 mg $230.00 $0.00
10 mg $408.00 $0.00
25 mg $893.00 $0.00
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Cart Total $0.00

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Pricing updated 2014-04-17. Prices are subject to change without notice.

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