| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg | |||
| 50mg | |||
| 100mg | |||
| 250mg | |||
| 500mg |
| Targets |
Beta-3 adrenergic receptor (β3-AR). Amibegron hydrochloride is a selective agonist of the β3-AR. Activation of this receptor leads to the stimulation of adenylate cyclase, increasing intracellular cAMP levels. This results in the relaxation of smooth muscle, particularly in the urinary bladder, and has metabolic effects such as increasing thermogenesis and lipolysis.
|
|---|---|
| ln Vitro |
Amibegron Hydrochloride (SR 58611A) is a selective beta-adrenoceptor agonist having an EC50 of 3.5 nM at beta-adrenergic receptors in rat colon and an EC50 of 499 nM in rat uterus[1]. Amibegron Hydrochronide (SR 58611A) has little effect on β1- and β2-adrenergic receptors, 5-HT uptake, norepinephrine (NA) uptake, and dopamine (DA) uptake in rat brain tissue, with IC50 of 4.6 respectively. and 1.2, 0.58, 2.5 and 3.2μM respectively; no effect on 5-HT1A, 5-HT2, MAO-A and MAO-B (IC50 > 10 μM) [2].
Amibegron hydrochloride is a potent and selective β3-adrenergic receptor agonist. It has been shown to relax bladder smooth muscle in vitro. Its selectivity for β3-AR over β1- and β2-AR has been demonstrated in binding and functional assays. It has been investigated for its effects on bladder function and its potential to treat overactive bladder. |
| ln Vivo |
Amibegron Hydrochronide (SR 58611A, 0.1 to 0.3 mg/kg, intraperitoneally) increases the toxicity of yohimbine in mice. In a rat model of learned helplessness, amibellone hydrochloride (0.6 and 2 mg/kg, i.p.) also exhibits antidepressant-like effects. However, at dosages as high as 10 mg/kg in mice and as high as 30 mg/kg in rats, amiberon hydrochloride has no effect on spontaneous locomotor activity [2]. Multiple rat brain regions (e.g., cortex, hippocampus, hypothalamus, striatum) had increased levels of 5-HT and tryptophan (Trp) production when administered amiberon hydrochloride (3 and 10 mg/kg, p.o.). Furthermore, oral Amibegron Hydrochronide (10 mg/kg) stimulates the release of 5-HT in the rat prefrontal cortex. Rats' dorsal raphe nucleus's serotonergic neurons remain unaffected by systemic (3 mg/kg, intravenous injection) or long-term (10 mg/kg, oral) SR58611A administration [3].
In vivo, Amibegron hydrochloride has been studied in animal models of overactive bladder, where it has been shown to increase bladder capacity and reduce urinary frequency. It has also been investigated for its potential antidepressant effects in animal models. Its effects are mediated through activation of the β3-AR. |
| Enzyme Assay |
In vitro receptor binding assays for Amibegron hydrochloride are performed using membrane preparations from cells expressing β3-AR. The compound is incubated with a radiolabeled ligand specific for β3-AR. Functional assays measure the activation of adenylate cyclase, with cAMP accumulation as the readout. Selectivity over β1- and β2-AR is assessed in similar assays.
|
| Cell Assay |
In vitro cell-based assays for Amibegron hydrochloride are performed using cells expressing the β3-AR, such as certain smooth muscle cell lines or recombinant cell lines. Cells are treated with the compound, and cAMP levels are measured. The compound's ability to relax smooth muscle can be assessed in isolated tissue preparations.
|
| Animal Protocol |
In vivo animal studies for Amibegron hydrochloride are conducted in models of overactive bladder. The compound is administered to rodents, and cystometry is performed to measure bladder capacity, voiding pressure, and urinary frequency. Its effects on depression-like behavior can be assessed in models such as the forced swim test.
|
| ADME/Pharmacokinetics |
Amibegron hydrochloride has a molecular weight of 469.38 and a molecular formula of C22H25ClN2O3S · HCl. As a hydrochloride salt, it is expected to have good aqueous solubility. It should be stored as powder at -20°C. For in vivo administration, it can be dissolved in saline or other suitable vehicles.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are documented for Amibegron hydrochloride in the provided sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound.
|
| References |
|
| Additional Infomation |
Amibegron hydrochloride is a potent and selective beta-3 adrenergic receptor agonist. It has been investigated for the treatment of overactive bladder, irritable bowel syndrome, and depression. Its selectivity for β3-AR over other beta-adrenergic receptors is a key feature. It is for research use only.
|
| Molecular Formula |
C22H26NO4CL.HCL
|
|---|---|
| Molecular Weight |
440.36008
|
| Exact Mass |
439.132
|
| CAS # |
121524-09-2
|
| PubChem CID |
121888
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
576ºC at 760mmHg
|
| Flash Point |
302.2ºC
|
| Vapour Pressure |
4.14E-14mmHg at 25°C
|
| LogP |
4.655
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
29
|
| Complexity |
491
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CCOC(=O)COC1=CC2=C(CC[C@@H](C2)NC[C@@H](C3=CC(=CC=C3)Cl)O)C=C1.Cl
|
| InChi Key |
NQIZCDQCNYCVAS-RQBPZYBGSA-N
|
| InChi Code |
InChI=1S/C22H26ClNO4.ClH/c1-2-27-22(26)14-28-20-9-7-15-6-8-19(11-17(15)12-20)24-13-21(25)16-4-3-5-18(23)10-16;/h3-5,7,9-10,12,19,21,24-25H,2,6,8,11,13-14H2,1H3;1H/t19-,21-;/m0./s1
|
| Chemical Name |
ethyl 2-[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydronaphthalen-2-yl]oxy]acetate;hydrochloride
|
| 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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~227.09 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.68 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 (5.68 mM) (saturation unknown) in 10% DMSO + 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 25.0 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: ≥ 2.5 mg/mL (5.68 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 | 2.2709 mL | 11.3543 mL | 22.7087 mL | |
| 5 mM | 0.4542 mL | 2.2709 mL | 4.5417 mL | |
| 10 mM | 0.2271 mL | 1.1354 mL | 2.2709 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.
Efficacy and Safe
An 8-week, double blind, placebo-controlled, multicenter study with paroxetine (20 mg q24) as positive control, evaluating the efficacy and safety of 2 fixed doses of SR58611A (175 mg q12 and 350 mg q12) in outpatients with Generalized Anxiety Disorder.
CTID: null
Phase: Phase 3 Status: Completed
Date: 2006-02-02
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
