Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
Ambrisentan (formerly BSF-208075; LU-208075; BSF208075; LU208075; Letairis; Volibris; pulmonext) is a selective antagonist of the endothelin-1 type A receptor (ETA). For the treatment of pulmonary hypertension, ambrisentan has received FDA approval.
Targets |
ETA receptor
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
Cell Assay |
Cells are randomly assigned to four groups for every BMEC experiment, unless otherwise specified: (1) normoxia vehicle control (Nx-CTRL); (2) normoxia-treated; (3) hypoxia (24 h) control (Hx-CTRL); and (4) hypoxia (24 h) treated. Nrf2 activators are added 24 hours before any hypoxic exposures, as previously mentioned. Protandim (100 μg/mL), methazolamide (125 μg/mL), nifedipine (7 μg/mL), or ambrisentan (40 μg/mL) are the cell treatments. Additionally, Nrf2 siRNA is applied to a subset of cells. In these tests, siRNA is added 24 hours before medication administration. The purpose of the 24-hour hypoxia exposure for BMEC is to guarantee that the cells maintain their siRNA transfection both during the 24-hour hypoxia exposure and during the drug pre-treatment (24 hours in normoxia). On three different days (n=9), data is gathered from a minimum of three distinct cell culture preparations[2].
|
|
Animal Protocol |
|
|
References |
Molecular Formula |
C22H22N2O4
|
---|---|
Molecular Weight |
378.42
|
Exact Mass |
378.16
|
Elemental Analysis |
C, 69.83; H, 5.86; N, 7.40; O, 16.91
|
CAS # |
177036-94-1
|
Related CAS # |
Ambrisentan sodium; 1386915-48-5; Ambrisentan-d10; 1046116-27-1
|
Appearance |
Solid powder
|
SMILES |
CC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C
|
InChi Key |
OUJTZYPIHDYQMC-LJQANCHMSA-N
|
InChi Code |
InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
|
Chemical Name |
(2S)-2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
|
Synonyms |
LU-208075; BSF-208075; BSF208075; LU208075; BSF 208075; LU 208075; trade name Letairis; Volibris; pulmonext
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 0.71 mg/mL (1.88 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.71 mg/mL (1.88 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix well. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: 10% EtOH + 90% Corn Oil Solubility in Formulation 6: 12.5 mg/mL (33.03 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL | |
5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | |
10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05437224 | Completed | Drug: Ambrisentan | Pulmonary Arterial Hypertension | RenJi Hospital | December 18, 2018 | Phase 3 |
NCT01330108 | Completed | Drug: ambrisentan | Pulmonary Arterial Hypertension | University of Alabama at Birmingham | May 2011 | Phase 4 |
NCT01072669 | Completed | Drug: ambrisentan | Ischemia | Soumya Chatterjee | February 2010 | Not Applicable |
NCT01224210 | Completed | Drug: Ambrisentan | Portopulmonary Hypertension | Tufts Medical Center | March 2010 | Phase 3 |
Histological analyses of liver tissues. Representative images of hematoxylin-eosin staining (magnification, × 100) in the (A) control and (B) ambrisentan groups; representative images of oil red O staining (magnification, × 100) in the (C) control and (D) ambrisentan groups; E: The proportion (%) of the hepatic steatosis area stained with oil red O was measured using image analysis. World J Hepatol . 2016 Aug 8;8(22):933-41. td> |
Immunohistochemistry overlay of Nrf2 activation in rats treated for 4 days with vehicle control, acetazolamide (40 mg/kg), verapamil (10mg/kg), Protandim (10 mg/kg), methazolamide (4 mg/kg), nifedipine (2 mg/kg), or ambrisentan (1 mg/kg). Free Radic Biol Med . 2013 Oct:63:264-73. td> |
Analysis of Nrf2 nuclear concentration in Bovine Brain Microvascular Endothelial (BMEC) cells treated for 24 h with Protandim (125 μg/mL), methazolamide (100 μg/mL), nifedipine (7.5 μg/mL), or ambrisentan (40 μg/mL). Free Radic Biol Med . 2013 Oct:63:264-73. td> |