Nelociguat (BAY60-4552) (Synonyms: BAY 60-4552, Desmethyl Riociguat) |
| Catalog No.GC32493 |
Nelociguat (BAY60-4552) (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 625115-52-8
Sample solution is provided at 25 µL, 10mM.
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Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway[1]. Riociguat is metabolized to BAY60-4552 not only via cytochrome P450 isoenzymes 3A4 (CYP3A4), CYP2C8, and CYP2J2, but also via CYP1A1, located in the liver and lungs[2].
GSK2181236A and BAY 60-4552 provide partial benefit against hypertension-induced end-organ damage. In spontaneously hypertensive stroke-prone rats, a low dose of BAY 60-4552 decreases urine output and improved survival. A high dose also reduces urine output, and in addition reduces microalbuminuria and attenuates the increase in mean arterial pressure. Both the 0.3 and 3 mg/kg/day doses of BAY 60-4552 improves survival of 46 and 69%. Seven weeks of treatment with BAY 60-4552 (0.3 and 3.0 mg/kg/day) dose-dependently decreases urine output to 79±11 and 56±10 mL/day[1]. BAY 60-4552, and vardenafil provides synergistic beneficial effects and might therefore salvage patients who experience treatment failures with PDE5 inhibitors after radical prostatectomy[3].
[1]. Costell MH, et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. [2]. Zhao X, et al. Pharmacokinetics of the Soluble Guanylate Cyclase Stimulator Riociguat in Healthy Young Chinese Male Non-Smokers and Smokers: Results of a Randomized, Double-Blind, Placebo-Controlled Study. Clin Pharmacokinet. 2016 May;55(5):615-24. [3]. Oudot A, 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. 2011 Nov;60(5):1020-6.
Animal experiment: | Rats: Rats are orally gavaged with vehicle (0.5% HPMC, 5% DMSO, and 0.1% Tween 80; 10 mL/kg; n=14), GSK2181236A (0.1 or 1.0 mg/kg; n=11-14), or BAY 60-4552 (0.3 or 3.0 mg/kg; n=10-12) 2 h prior to ischemia. Blood is collected at the initiation of ischemia and after 24 h reperfusion. Plasma is obtained for analysis[1]. |
References: [1]. Costell MH, et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. | |
| Cas No. | 625115-52-8 | SDF | |
| Synonyms | BAY 60-4552, Desmethyl Riociguat | ||
| Canonical SMILES | O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)N=C1N | ||
| Formula | C19H17FN8O2 | M.Wt | 408.39 |
| Solubility | DMSO : 105 mg/mL (257.11 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4486 mL | 12.2432 mL | 24.4864 mL |
| 5 mM | 0.4897 mL | 2.4486 mL | 4.8973 mL |
| 10 mM | 0.2449 mL | 1.2243 mL | 2.4486 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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