BAY-747
Based on 1 Customer Validation
BAY-747 (BAY 1165747) is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model.
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- Purity: 98.01%
- CAS No.: 1609342-18-8
- 화학식: C22H26F2N4O2
- 분자량:416.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
Soluble guanylate cyclase (sGC)[1]
BAY-747 (100 nM) enhances AMPA receptor dynamics in an ex vivo acquisition-like cLTP model, in combination with WS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ex vivo acquisition-like cLTP model
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Concentration:100 nM
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Incubation Time:
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Result:Increased the phosphorylation levels of S845 on GluA1.
BAY-747 (0.03-1.0 mg/kg,2 mL/kg ; po; 30 min before T1 in a 24 h interval OLT) enhance long-term memory acquisition processes in rat object location task (OLT) model, and also attenuates L-NAME induced short-term memory impairments. BAY-747 does not affect GluA1-containing AMPAR dynamics in the hippocampus[1].
BAY-747 (0.003-0.3 mg/kg; po; single dose) decreases blood pressure in rats, and also (3 mg/kg; po; once daily for 35 days) increases body weight of rats in l-NAME-Treated Renin Transgenic model[2].
BAY-747 (150 mg/kg of food; po; 16 weeks) improves grip strength and running speed in male mdx/mTRG2 mice, suggesting improved skeletal muscle function[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat object location task (OLT) model[1]
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Dosage:0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
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Administration:PO; 30 min before T1 in a 24 h interval OLT
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Result:Resulted significantly higher long-term memory performance at 0.03, 0.1, 0.3 and 1.0 mg/kg dose, 30 min before T1.
Attenuated L-NAME induced short-term memory impairments at 0.3 mg/kg and 1 mg/kg.
Did not enhance GluA1 trafficking at 1 mg/kg 24 h after treatment.
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Animal Model:Anesthetized, conscious spontaneously hypertensive and conscious normotensive rats[2]
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Dosage:0 mg/kg, 0.003 mg/kg, 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, and 0.3 mg/kg
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Administration:IV; single dose
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Result:Produced a dose-dependent and long-lasting decrease in blood pressure in rats.
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Animal Model:l-NAME-Treated Renin Transgenic Rats[2]
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Dosage:0.3 mg/kg, 3 mg/kg
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Administration:PO; once daily for 35 days; l-NAME treatment: 30 mg/kg, po, for 6 days
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Result:Resulted a significant weight gain among rats.
Led to a dose-dependent increase of plasma cGMP. Decreased blood pressure only at 3 mg/kg.
Chemical Information
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CAS No. 1609342-18-8
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Appearance Solid
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분자량 416.46
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화학식 C22H26F2N4O2
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Color White to off-white
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SMILES
FC(C=CC=C1F)=C1COC2=CC(C)=CN3C2=NC(C)=C3C(NC[C@@](C)(N)CC)=O
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Synonyms
BAY 1165747
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Nelissen E, et al. 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. [Content Brief]
[2]. Vakalopoulos A, et al. 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. [Content Brief]
[3]. Krishnan SM, et al. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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