| Field | Specification |
|---|---|
| Target | |
| Alternative names | SKF-9976 citrate; AF-438 citrate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H27N3O8 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Oxolamine citrate, also known as SKF-9976 citrate or AF-438 citrate, is an orally active antitussive that can inhibit CYP2B1/2. It has anti-inflammatory effects on the respiratory organs of guinea pigs, increases the AUC of Warfarin, and prolongs its terminal half-life. It can be used in respiratory disease research[1][2][3][4]. It is supplied as a white to off-white solid (C20H27N3O8, MW 437.44) at 99.87% purity.
Physical & Chemical Properties
| CAS Number | 1949-20-8 |
|---|---|
| Molecular Formula | C20H27N3O8 |
| Molecular Weight | 437.44 g/mol |
| Purity | 99.87% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CCN(CC)CCC1=NC(C2=CC=CC=C2)=NO1.O=C(CC(C(O)=O)(O)CC(O)=O)O |
| Target | CYP2B1, CYP2B2 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: ≥ 100 mg/mL (228.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 14.29 mg/mL (32.67 mM; Requires sonication) * "≥" means soluble, but saturation unknown. |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 100 mg/mL (228.60 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 14.29 mg/mL (32.67 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | PBS |
|---|---|
| Result | 28 mg/mL (64.01 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
In fresh rat plasma, Oxolamine (10 μg/mL; 24 h) citrate significantly lowers the plasma protein binding of Clarithromycin[3].
In Vivo
In male SD rats, Oxolamine citrate (10-50 mg/kg; p.o.; 3 times daily for 3 consecutive days) significantly raises the AUC and extends the terminal half-life of Warfarin[3]. Oxolamine citrate (initially 80 mg/kg body weight, then 53.3 mg/kg; i.p.; administered 11 times at 3, 6, 9, 24, 28 and 32, then 48, 52, 56, 72 and 76 h) produces a distinct anti-inflammatory effect on the respiratory organs of guinea pigs[4].
| Animal Model | Guinea pigs + non-bacterial inflammation of the respiratory tract model induced by inhalation of acrolein aerosol[4] |
|---|---|
| Dosage | 80 mg/kg body weight initially, then 53.3 mg/kg |
| Administration | Intraperitoneal injection, 11 times at 3, 6, 9, 24, 28, 32, 48, 52, 56, 72 and 76 h |
| Result | Reduced relative lung weight. Significantly reduced inflammation levels. Protected the pulmonary parenchyma from emphysema. Showed anti-inflammatory effect superior to that of Phenylbutyrone. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
