| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Aladorian targets the ryanodine receptor (RyR), specifically the cardiac isoform RyR2. It acts as a potent blocker of RyR2 and also modulates RyR1 and RyR3. By stabilizing the RyR2 channel, it prevents aberrant calcium release from the sarcoplasmic reticulum, which is implicated in arrhythmias and heart failure.
|
|---|---|
| ln Vitro |
In vitro, Aladorian acts as a potent blocker of ryanodine receptor 2 (RyR2) and also modulates RyR1 and RyR3. Its activity has been characterized in calcium release assays measuring RyR channel function. However, specific IC50 values are not provided in the available references.
|
| ln Vivo |
In vivo, Aladorian is used for the research of heart failure and catecholaminergic polymorphic ventricular tachycardia (CPVT). Its anti-arrhythmia effects have been demonstrated in preclinical models. However, specific animal model data are not provided in the available references.
|
| Enzyme Assay |
In vitro receptor binding assays for Aladorian measure its activity at the ryanodine receptor (RyR), specifically RyR2. These cell-based or membrane-based systems assess the compound's ability to modulate RyR-mediated calcium release. Functional assays measure calcium flux in response to RyR activation.
|
| Cell Assay |
In vitro cellular assays for Aladorian involve the use of cardiomyocytes to measure its effects on calcium handling and arrhythmogenesis. Cells are treated with the compound, and calcium transients, sarcoplasmic reticulum calcium content, and spontaneous calcium release events are assessed.
|
| Animal Protocol |
In vivo animal studies for Aladorian have been conducted in models of heart failure and catecholaminergic polymorphic ventricular tachycardia (CPVT). Animals are treated with the compound, and cardiac function, arrhythmia incidence, and survival are assessed. However, specific protocols and detailed results are not provided.
|
| References |
[3]. Analytical approaches for the detection of emerging\ntherapeutics and non-approved drugs in human doping controls. J Pharm Biomed\nAnal. 2014 Dec;1066-83. |
| Molecular Formula |
C12H13NO4S
|
|---|---|
| Molecular Weight |
267.30092215538
|
| Exact Mass |
267.057
|
| CAS # |
865433-00-7
|
| Related CAS # |
865433-00-7 (free acid);1233219-11-8 (sodium);
|
| PubChem CID |
11161474
|
| Appearance |
White to light yellow solid powder
|
| LogP |
1.152
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
336
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C(N1CCSC2C(=CC(=CC=2)OC)C1)=O)O
|
| InChi Key |
FPWBHFYYVSNIFZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H13NO4S/c1-17-9-2-3-10-8(6-9)7-13(4-5-18-10)11(14)12(15)16/h2-3,6H,4-5,7H2,1H3,(H,15,16)
|
| Chemical Name |
(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)oxoacetic acid
|
| Synonyms |
ARM036 ARM-036 ARM 036 S36 S-36 S44121-1 S44121-1
|
| 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) |
DMSO : ~105 mg/mL (~392.82 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (19.64 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 52.5 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: 5.25 mg/mL (19.64 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 52.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 5.25 mg/mL (19.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7411 mL | 18.7056 mL | 37.4111 mL | |
| 5 mM | 0.7482 mL | 3.7411 mL | 7.4822 mL | |
| 10 mM | 0.3741 mL | 1.8706 mL | 3.7411 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
