Ambrisentan-d3 |
Catalog No.GC49638
One-Click Copy Product Info
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An internal standard for the quantification of ambrisentan
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1189479-60-4
Sample solution is provided at 25 µL, 10mM.
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Ambrisentan-d3 is intended for use as an internal standard for the quantification of ambrisentan by GC- or LC-MS. Ambrisentan is a nonpeptide endothelin A (ETA) receptor antagonist (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively).1 It inhibits contraction of isolated rabbit aortic rings induced by endothelin-1 by 43.23% when used at a concentration of 1 µM.2 Ambrisentan inhibits ET-1-induced contraction of human pulmonary and radial arteries in vitro (Kd = 0.042 and 0.11 μM, respectively).3 In a rat model of neonatal hyperoxic lung injury, ambrisentan (20 mg/kg per day, s.c.) reduces pulmonary arterial hypertension (PAH) as well as decreases PAH-induced right ventricular hypertrophy (RVH) and peak RV pressure.4 Formulations containing ambrisentan have been used in the treatment of PAH.
1.Yokoyama, Y., Osano, A., Hyashi, H., et al.Endothelin-1 receptors in rat tissues: Characterization by bosentan, ambrisentan and CI-1020Biol. Pharm. Bull.37(3)461-465(2014) 2.Xia, J., Song, J., Zhen, L., et al.Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonistsBioorg. Med. Chem. Lett.21(13)3894-3897(2011) 3.Angus, J.A., Soeding, P.F., Hughes, R.J.A., et al.Functional estimation of endothelin-1 receptor antagonism by bosentan, macitentan and ambrisentan in human pulmonary and radial arteries in vitroEur. J. Pharmacol.804111-116(2017) 4.Wagenaar, G.T., Laghmani, e.H., de Visser, Y.P., et al.Ambrisentan reduces pulmonary arterial hypertension but does not stimulate alveolar and vascular development in neonatal rats with hyperoxic lung injuryAm. J. Physiol. Lung Cell Mol. Physiol.304(4)L264-L275(2013)
| Cas No. | 1189479-60-4 | SDF | |
| Canonical SMILES | CC1=NC(OC(C(O)=O)C(OC([2H])([2H])[2H])(C2=CC=CC=C2)C3=CC=CC=C3)=NC(C)=C1 | ||
| Formula | C22H19D3N2O4 | M.Wt | 381.4 |
| Solubility | DMSO: soluble | Storage | -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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6219 mL | 13.1096 mL | 26.2192 mL |
| 5 mM | 524.4 μL | 2.6219 mL | 5.2438 mL |
| 10 mM | 262.2 μL | 1.311 mL | 2.6219 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 10 reference(s) in Google Scholar.)