YS-201 |
Katalog-Nr.GC32648
One-Click Copy Product Info
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YS-201 ist ein Calciumkanal-Antagonist vom Dihydropyridin-Typ.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 108852-42-2
Sample solution is provided at 25 µL, 10mM.
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YS-201 is a dihydropyridine-type calcium channel antagonist previously in clinical trials for the treatment of angina pectoris and hypertension.
YS-201 (Diperdipine) markedly reduces systemic vascular resistance and improves stroke index and left ventricular ejection fraction. Mean pulmonary artery and wedge pressures are slightly increased as a possible consequence of enhanced venous return, whereas right atrial and left ventricular end-diastolic pressures are not significantly changed. Nevertheless, an increase in preload is clearly indicated by an augmented left ventricular end-diastolic volume index after administration of diperdipine[1]. After intravenous and oral doses, absolute bioavailability is calculated to be 18.7%. Biliaryexcretion accounts for about 0.1% of the total clearance of diperdipine and does not contribute to the overall elimination of the drug. After intraportal administration, the bioavailable fraction of diperdipine is increasing up to 44.3% suggesting a prehepatic site of loss of the drug[2]. The single application of diperdipine to mice and rats by gavage causes intolerance reactions starting at the lowest tested dose level of 200 mg/kg b.w. p.o. (mice) and at 250 mg/kg b.w. p.o. (rats). In the rat, toxic effects occur from 15 mg diperdipine/kg b.w./day p.o. onwards[3].
[1]. Di Donato M, et al. Acute hemodynamic effects of intravenous diperdipine, a new dihydropyridine derivative, in coronary heart disease. Am Heart J. 1991 Mar;121(3 Pt 1):776-81. [2]. Greiner PO, et al. Evaluation of first pass effect and biliary excretion of diperdipine in the dog. Eur J Drug Metab Pharmacokinet. 1990 Jul-Sep;15(3):185-90. [3]. Herzog R, et al. Experimental studies on the toxicity of diperdipine following oral and parenteral application. Arzneimittelforschung. 1995 Mar;45(3):240-5.
| Cas No. | 108852-42-2 | SDF | |
| Canonical SMILES | O=C(C1=C(C)NC(C)=C(C(OCCN2CCCCC2)=O)C1C3=CC=CC([N+]([O-])=O)=C3)OCC | ||
| Formula | C24H31N3O6 | M.Wt | 457.52 |
| Löslichkeit | Soluble in DMSO | 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 | 2.1857 mL | 10.9285 mL | 21.857 mL |
| 5 mM | 437.1 μL | 2.1857 mL | 4.3714 mL |
| 10 mM | 218.6 μL | 1.0928 mL | 2.1857 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 saline, 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)