| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 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].
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| 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].
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| References |
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| Molecular Formula |
C22H26NO4CL.HCL
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|---|---|
| Molecular Weight |
440.36008
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| Exact Mass |
439.132
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| CAS # |
121524-09-2
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| PubChem CID |
121888
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| Appearance |
White to off-white solid powder
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| Boiling Point |
576ºC at 760mmHg
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| Flash Point |
302.2ºC
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| Vapour Pressure |
4.14E-14mmHg at 25°C
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| LogP |
4.655
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
491
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCOC(=O)COC1=CC2=C(CC[C@@H](C2)NC[C@@H](C3=CC(=CC=C3)Cl)O)C=C1.Cl
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| InChi Key |
NQIZCDQCNYCVAS-RQBPZYBGSA-N
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| 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
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| Chemical Name |
ethyl 2-[[(7S)-7-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-5,6,7,8-tetrahydronaphthalen-2-yl]oxy]acetate;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~227.09 mM)
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|---|---|
| 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
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