A stimulator of soluble guanylate cyclase and an active metabolite of riociguat
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Parent Compound(s)
9000554Riociguat
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Nelociguat

Item No. 34133

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-carbamic acid, methyl ester
CAS Number
625115-52-8
Synonyms
  • BAY 60-4552
  • Desmethyl Riociguat
Molecular Formula
C19H17FN8O2
Formula Weight
408.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: slightly, heatedMethanol: very slightly, heated
SMILES
O=C(NC1=C(N)N=C(C2=NN(CC3=C(F)C=CC=C3)C4=C2C=CC=N4)N=C1N)OC
InChi Code
InChI=1S/C19H17FN8O2/c1-30-19(29)24-14-15(21)25-17(26-16(14)22)13-11-6-4-8-23-18(11)28(27-13)9-10-5-2-3-7-12(10)20/h2-8H,9H2,1H3,(H,24,29)(H4,21,22,25,26)
InChi Key
FTQHGWIXJSSWOY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $95

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    10 mg

    $168

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    25 mg

    $279

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    50 mg

    $417

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    Product Description

    Nelociguat is a stimulator of soluble guanylate cyclase (sGC) and an active metabolite of riociguat (Item No. 9000554).1,2 It is formed from riociguat by the cytochrome P450 (CYP) isoform CYP1A1.3 Nelociguat increases phosphorylation of the protein kinase G (PKG) substrate vasodilator-stimulator protein (VASP) in isolated rat aortic smooth muscle cells (EC50 = 353 nM).1 It induces vasodilation in rat aortic rings (EC50 = 75 nM). Nelociguat (3 mg/kg) decreases urine output and cardiac hypertrophy, as well as improves survival, in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet. It improves erectile responses to electrical stimulation of the cavernous nerve in a rat model of cavernous nerve crush injury when administered at doses of 0.03 and 0.3 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Costell, M.H., Ancellin, N., Bernard, R.E., et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front. Pharmacol. 3, 128 (2012).

    2. Oudot, A., Behr-Roussel, D., Poirier, S., et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: A proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur. Urol. 60(5), 1020-1026 (2011).

    3. Hložek, T., Štícha, M., Bursová, M., et al. Sensitive CE-MS method for monitoring of riociguat and desmethylriociguat levels in human serum. Electrophoresis 41(18-19), 1564-1567 (2020).