Vericiguat (BAY1021189, Verquvo) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ACTIVATOR
Mechanism of action
Soluble guanylate cyclase activator
Product Description
Information
Vericiguat Vericiguat (BAY1021189, Verquvo) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator.
Targets
sGC
In vitro
The stimulation of sGC by Vericiguat is examined with a recombinant CHO cell line overexpressing rat sGC. Vericiguat stimulates the sGC reporter cell line concentration dependently with an EC50 of 1005 ± 145 nM. In the presence of the NO donor S-nitroso-N-acetyl-D,L-penicillamine (SNAP) (30 and 100 nM), the EC50 value shifts to 39.0 ± 5.1 and 10.6 ± 1.7 nM, respectively. In the presence of ODQ, pretreatment of the sGC reporter cell line with 10 μM ODQ for 3 h results in a significantly reduced efficacy of Vericiguat, with an EC50 of 256 ± 40 nM being observed.
In vivo
Vericiguat can maintain heart and kidney function in a model of hypertension-induced end-organ damage with substantially reduced overall mortality.
1.Follmann M, Ackerstaff J, Redlich G, Wunder F, Lang D, Kern A, Fey P, Griebenow N, Kroh W, Becker-Pelster EM et al.. (2017) Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.. J Med Chem, 60 (12):(5146-5161). [PMID:28557445][10.1021/op500134e]
2.Pieske B, Butler J, Filippatos G, Lam C, Maggioni AP, Ponikowski P, Shah S, Solomon S, Kraigher-Krainer E, Samano ET et al.. (2014) Rationale and design of the SOluble guanylate Cyclase stimulatoR in heArT failurE Studies (SOCRATES).. Eur J Heart Fail, 16 (9):(1026-38). [PMID:25056511][10.1021/op500134e]
3.Armstrong PW, Roessig L, Patel MJ, Anstrom KJ, Butler J, Voors AA, Lam CSP, Ponikowski P, Temple T, Pieske B et al.. (2018) A Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial of the Efficacy and Safety of the Oral Soluble Guanylate Cyclase Stimulator: The VICTORIA Trial.. JACC Heart Fail, 6 (2):(96-104). [PMID:29032136][10.1021/op500134e]
4.Lam CSP, Giczewska A, Sliwa K, Edelmann F, Refsgaard J, Bocchi E, Ezekowitz JA, Hernandez AF, O'Connor CM, Roessig L et al.. (2020) Clinical Outcomes and Response to Vericiguat According to Index Heart Failure Event: Insights From the VICTORIA Trial.. JAMA Cardiol, 71 (13):(1755-70). [PMID:33185650][10.1021/op500134e]
5.Butler J, Lam CSP, Anstrom KJ, Ezekowitz J, Hernandez AF, O'Connor CM, Pieske B, Ponikowski P, Shah SJ, Solomon SD et al.. (2019) Rationale and Design of the VITALITY-HFpEF Trial.. Circ Heart Fail, 12 (5):(e005998). [PMID:31096775][10.1021/op500134e]
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