| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1] EC50: 8.6±0.77 nM (human GABAB receptor)[1]
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|---|---|
| ln Vitro |
Human islet cell proliferation is enhanced in vitro by leogaberan hydrochloride (3–30 nM)[2].
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| ln Vivo |
In dogs, lesogaberan hydrochloride shows a biphasic dose-response curve that potently activates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR)[1]. Apoptosis of human islet β-cells in islet grafts in mice is prevented by oral Lesogaberan hydrochloride (0.08 mg/mL; 48 hours)[2]. Sprague-Dawley female rats exhibit relatively low systemic clearance and high oral availability (88% in the dog and 100% in the rat) when given lesogaberan (7 μmol/kg) hydrochloride[1].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Human islet cells Tested Concentrations: 3, 10, and 30 nM Incubation Duration: 4 days Experimental Results: Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone. |
| Animal Protocol |
Animal/Disease Models: Diabetic NOD/SCID (severe combined immunodeficient) mouse were implanted with human islets[2]
Doses: 0.08 mg/mL Route of Administration: 48 hrs (hours) Experimental Results: Dramatically decreased the percentages of apoptotic islet cells and increased the frequency of insulin+ β-cells in human islet grafts. Animal/Disease Models: Female Sprague Dawley rats[1] Doses: 7 μmol/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral Experimental Results: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma. |
| References |
|
| Molecular Formula |
C3H9CLFNO2P
|
|---|---|
| Molecular Weight |
176.534224271774
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| Exact Mass |
176.004
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| CAS # |
2925644-17-1
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| Related CAS # |
Lesogaberan;344413-67-8;Lesogaberan napadisylate;477956-38-0
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| PubChem CID |
162640398
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| Appearance |
Colorless to light yellow viscous liquid
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
9
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| Complexity |
89.4
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
Cl.[P+](C[C@@H](CN)F)(=O)O
|
| InChi Key |
CJVIVHIKWIZWOJ-AENDTGMFSA-O
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| InChi Code |
InChI=1S/C3H7FNO2P.ClH/c4-3(1-5)2-8(6)7;/h3H,1-2,5H2;1H/p+1/t3-;/m1./s1
|
| Chemical Name |
[(2R)-3-amino-2-fluoropropyl]-hydroxy-oxophosphanium;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 (e.g. under nitrogen), 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: 240 mg/mL (1351.81 mM)
H2O: 100 mg/mL (563.25 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6 mg/mL (33.80 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 60.0 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: ≥ 6 mg/mL (33.80 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 60.0 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: ≥ 6 mg/mL (33.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (563.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.6648 mL | 28.3238 mL | 56.6476 mL | |
| 5 mM | 1.1330 mL | 5.6648 mL | 11.3295 mL | |
| 10 mM | 0.5665 mL | 2.8324 mL | 5.6648 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.
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