| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
α-Adrenergic receptors (α1A-AR and α1B-AR). Buflomedil HCl is an α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. It also inhibits phosphodiesterase activity, leading to increased intracellular cAMP levels, and inhibits platelet aggregation.
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|---|---|
| ln Vitro |
Buflomedil HCl binds to rat α1A- and α1B-ARs with Kis of 4.06 and 6.84 µM, respectively. It enhances intracellular cAMP levels in human keratinocytes, either secondary to adenyl-cyclase stimulation or phosphodiesterase inhibition. The compound leads to a weak inhibition of collagen- and ADP-induced platelet aggregation. It also exhibits weak calcium antagonistic effects and oxygen-sparing activity.
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| ln Vivo |
In vivo, buflomedil HCl acts as a peripheral vasodilating agent, improving blood flow by dilating peripheral blood vessels and enhancing microcirculation. It has been used in the investigation of peripheral arterial disease, ischemia, intermittent claudication, and vascular pathologies. The compound is orally active and has been studied for its protective effects in models of cerebral ischemia.
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| Enzyme Assay |
In vitro enzyme assays for buflomedil HCl involve measuring its inhibition of phosphodiesterase activity or adrenergic receptor binding. Phosphodiesterase is incubated with cAMP and various concentrations of buflomedil HCl. cAMP hydrolysis is measured, and IC50 values are determined. Adrenergic receptor binding assays use radiolabeled ligands and membrane preparations from cells expressing α1A- or α1B-ARs.
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| Cell Assay |
In vitro cellular assays for buflomedil HCl involve treating cells (such as keratinocytes or vascular smooth muscle cells) with the compound and measuring cAMP levels, cell proliferation, or contraction. Cells are treated with various concentrations of buflomedil HCl, and cAMP levels are measured by ELISA. The compound's effects on cell function and signaling are assessed.
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| Animal Protocol |
In vivo animal studies for buflomedil HCl typically involve administration to rodent models of peripheral arterial disease, cerebral ischemia, or other vascular conditions. Efficacy is assessed by measuring blood flow, tissue perfusion, or functional outcomes. Buflomedil HCl has shown protective effects in a rat model of moderate cerebral ischemia.
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| ADME/Pharmacokinetics |
Buflomedil HCl is orally active and has a molecular weight of 343.85. It has been studied for its pharmacokinetic properties in biological samples using gas chromatographic-mass spectrometric analysis. The compound's pharmacokinetic profile supports its use in the investigation of peripheral and cerebral vascular diseases.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of buflomedil HCl have been conducted. The compound has been evaluated for its safety in various animal models. It is generally well tolerated at therapeutic doses. Comprehensive toxicological evaluation has been conducted to support its clinical use. The compound should be used under appropriate medical supervision.
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| References | |
| Additional Infomation |
4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone is an aromatic ketone.
Buflomedil HCl (buflomedil hydrochloride) is a vasodilator and non-selective α-adrenergic receptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. It improves blood flow by dilating peripheral blood vessels, enhancing microcirculation, and reducing blood viscosity. Buflomedil HCl is orally active and has been used in the investigation of peripheral arterial disease, intermittent claudication, and vascular pathologies. |
| Molecular Formula |
C17H26CLNO4
|
|---|---|
| Molecular Weight |
343.84
|
| Exact Mass |
343.155
|
| CAS # |
35543-24-9
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| Related CAS # |
Buflomedil;55837-25-7
|
| PubChem CID |
2467
|
| Appearance |
White to off-white solid powder
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| Boiling Point |
454.5ºC at 760 mmHg
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| Melting Point |
193°C
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| Flash Point |
228.7ºC
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| LogP |
3.511
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
22
|
| Complexity |
330
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
OWYLAEYXIQKAOL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H25NO4/c1-20-13-11-15(21-2)17(16(12-13)22-3)14(19)7-6-10-18-8-4-5-9-18/h11-12H,4-10H2,1-3H3
|
| Chemical Name |
4-pyrrolidin-1-yl-1-(2,4,6-trimethoxyphenyl)butan-1-one
|
| Synonyms |
Buflomedil Hydrochloride; Buflomedil HCl
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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)
|
| Solubility (In Vitro) |
H2O : ≥ 55 mg/mL (~159.95 mM)
DMSO : ~33.33 mg/mL (~96.93 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (8.00 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 27.5 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: ≥ 2.75 mg/mL (8.00 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 27.5 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: ≥ 2.75 mg/mL (8.00 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: 110 mg/mL (319.91 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 | 2.9083 mL | 14.5416 mL | 29.0833 mL | |
| 5 mM | 0.5817 mL | 2.9083 mL | 5.8167 mL | |
| 10 mM | 0.2908 mL | 1.4542 mL | 2.9083 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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