| Size | Price | |
|---|---|---|
| Other Sizes |
| ln Vivo |
The absorption mechanism of allisartan medoxomil is relatively easy. Allisartan medoxomil is entirely and directly transformed into EXP-3174 by esterase during the gastrointestinal absorption process [1]. Allisartan medoxomil (20, 80, and 320 mg/kg; interface; 26 weeks) decreases Sprague-Dawley weight growth at dosages of 80 to 320 mg/kg/day [1]. Allisartan isoproxil (30 mg/kg/day; lateral wall; 55 weeks) effectively lowers stroke susceptibility to renovascular hypertension
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|---|---|
| Animal Protocol |
Animal/Disease Models: Female and male SD (SD (Sprague-Dawley)) rats [1] Doses: 20, 80, and 320 mg/ kg dosing:
Experimental Results: diminished body weight gain (RHR-SP) and increased lifespan at 320 mg [2]. The dose for both sexes is /kg/day, and for women the dose is 80 mg/kg/day. At 80 and 320 mg/kg/day, men had diminished red blood cell parameters, diminished heart weight, and increased chronic progressive nephropathy (CPN) severity. |
| References |
|
| Molecular Formula |
C27H29CLN6O5
|
|---|---|
| Molecular Weight |
553.009364843369
|
| Exact Mass |
552.188
|
| CAS # |
947331-05-7
|
| PubChem CID |
24748496
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
745.0±70.0 °C at 760 mmHg
|
| Flash Point |
404.3±35.7 °C
|
| Vapour Pressure |
0.0±2.5 mmHg at 25°C
|
| Index of Refraction |
1.635
|
| LogP |
6.19
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
39
|
| Complexity |
786
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
XMHJQQAKXRUCHI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H29ClN6O5/c1-4-5-10-22-29-24(28)23(26(35)37-16-38-27(36)39-17(2)3)34(22)15-18-11-13-19(14-12-18)20-8-6-7-9-21(20)25-30-32-33-31-25/h6-9,11-14,17H,4-5,10,15-16H2,1-3H3,(H,30,31,32,33)
|
| Chemical Name |
propan-2-yloxycarbonyloxymethyl 2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~180.83 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.52 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 (4.52 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8083 mL | 9.0414 mL | 18.0829 mL | |
| 5 mM | 0.3617 mL | 1.8083 mL | 3.6166 mL | |
| 10 mM | 0.1808 mL | 0.9041 mL | 1.8083 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 |
| NCT06465264 | Completed | Drug: Allisartan Isoproxil/Amlodipine group 1
Drug: Amlodipine group 1 Drug: Allisartan Isoproxil/Amlodipine group 2 Drug: Allisartan Isoproxil group 2 |
Essential Hypertension | Shenzhen Salubris Pharmaceuticals Co., Ltd. | 2021-04-29 | Phase 3 |
| NCT06500689 | Completed | Drug: Allisartan Isoproxil/Sustained-Release Indapamide Drug: Allisartan Isoproxil |
Essential Hypertension | Shenzhen Salubris Pharmaceuticals Co., Ltd. | 2021-12-30 | Phase 3 |
| NCT02893358 | Unknown status | Drug: Allisartan Isoproxil Drug: Placebo |
Masked Hypertension | Yan Li | 2017-02-14 | Phase 4 |
| NCT04978649 | Withdrawn | Drug: Allisartan Isoproxil Drug: Amlodipine |
Blood Pressure Diabetes Mellitus, Type 2 |
Guangdong Provincial People's Hospital | 2021-09-01 | Phase 4 |
| NCT04111419 | Recruiting | Drug: Amlodipine/Atorvastatin 5 Mg-20 Mg ORAL TABLET Drug: Amlodipine/Atorvastatin 5 Mg-10 Mg ORAL TABLET Drug: Allisartan Isoproxil |
Atrial Fibrillation Hypertension |
Shanghai Jiao Tong University School of Medicine | 2020-07-01 | Phase 4 |
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