WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123205
CAS#: N/A
Description: BAY-1165747, also known as BAY-747, is a Long-Acting potent orally available sGC stimulator for the Treatment of Resistant Hypertension. BAY-747 showed the best overall profile in several in vitro and preclinically relevant in vivo experiments. It was selected as clinical candidate and the pharmacokinetic profile in humans was shown to be suitable for once-daily dosing by demonstrating a sustained effect on blood pressure and heart rate for up to 24 h.
Hodoodo Cat#: H123205
Name: BAY-1165747
CAS#: N/A
Chemical Formula: C22H26F2N4O2
Exact Mass: 416.20
Molecular Weight: 416.470
Elemental Analysis: C, 63.45; H, 6.29; F, 9.12; N, 13.45; O, 7.68
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Synonym: BAY-747; BAY747; BAY 747; BAY-1165747; BAY1165747; BAY 1165747
IUPAC/Chemical Name: (S)-N-(2-amino-2-methylbutyl)-8-((2,6-difluorobenzyl)oxy)-2,6-dimethylimidazo[1,2-a]pyridine-3-carboxamide
InChi Key: MITNUFZPBQIMAT-QFIPXVFZSA-N
InChi Code: InChI=1S/C22H26F2N4O2/c1-5-22(4,25)12-26-21(29)19-14(3)27-20-18(9-13(2)10-28(19)20)30-11-15-16(23)7-6-8-17(15)24/h6-10H,5,11-12,25H2,1-4H3,(H,26,29)/t22-/m0/s1
SMILES Code: O=C(C1=C(C)N=C2C(OCC3=C(F)C=CC=C3F)=CC(C)=CN21)NC[C@@](C)(N)CC
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 416.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension
Alexandros Vakalopoulos, Frank Wunder, Ingo V. Hartung, Gorden Redlich, Rolf Jautelat, Philipp Buchgraber, Jorma Hassfeld, Alexey V. Gromov, Niels Lindner, Donald Bierer, Jörg Gries, Walter Kroh, Holger Paulsen, Joachim Mittendorf, Dieter Lang, Eva Becker-Pelster, Damian Brockschnieder, Volker Geiss, Volkhart Li, Alexander Straub, Andreas Knorr, Thomas Mondritzki, Hubert Trübel, Marian Raschke, Martina Schaefer, Dirk Thomas, Peter Sandner, Johannes-Peter Stasch, and Markus Follmann
Journal of Medicinal Chemistry Article ASAP
DOI: 10.1021/acs.jmedchem.2c02082
1: Nelissen E, Possemis N, Van Goethem NP, Schepers M, Mulder-Jongen DAJ, Dietz
L, Janssen W, Gerisch M, Hüser J, Sandner P, Vanmierlo T, Prickaerts J. The sGC
stimulator BAY-747 and activator runcaciguat can enhance memory in vivo via
differential hippocampal plasticity mechanisms. Sci Rep. 2022 Mar 4;12(1):3589.
doi: 10.1038/s41598-022-07391-1. PMID: 35246566; PMCID: PMC8897390.
2: Krishnan SM, Nordlohne J, Dietz L, Vakalopoulos A, Haning P, Hartmann E,
Seifert R, Hüser J, Mathar I, Sandner P. Assessing the Use of the sGC Stimulator
BAY-747, as a Potential Treatment for Duchenne Muscular Dystrophy. Int J Mol
Sci. 2021 Jul 27;22(15):8016. doi: 10.3390/ijms22158016. PMID: 34360780; PMCID:
PMC8347633.
3: Vakalopoulos A, Wunder F, Hartung IV, Redlich G, Jautelat R, Buchgraber P,
Hassfeld J, Gromov AV, Lindner N, Bierer D, Gries J, Kroh W, Paulsen H,
Mittendorf J, Lang D, Becker-Pelster E, Brockschnieder D, Geiss V, Li V, Straub
A, Knorr A, Mondritzki T, Trübel H, Raschke M, Schaefer M, Thomas D, Sandner P,
Stasch JP, Follmann M. New Generation of sGC Stimulators: Discovery of
Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting
Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant
Hypertension. J Med Chem. 2023 Apr 11. doi: 10.1021/acs.jmedchem.2c02082. Epub
ahead of print. PMID: 37040336.