Choline theophyllinate
Based on 6 publication(s) in Google Scholar
Choline theophyllinate (Oxtriphylline) is an orally active methylxanthine derivative. Choline theophyllinate exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline theophyllinate relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. It modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline theophyllinate is used in studies of bronchospasm, nocturnal asthma, and chronic asthma.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 4499-40-5
- Formula: C12H21N5O3
- Molecular Weight:283.33
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Choline theophyllinate
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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RT-PCR
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In Vivo Efficacy Study
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RT-PCR
All Histamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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Human Endogenous Metabolite |
In Vitro
Choline theophyllinate (100 μg/mL; 15 min) causes concentration-dependent relaxation of isolated guinea-pig tracheal bronchial muscle and is used as a reference bronchodilator in this preparation[1].
Choline theophyllinate exhibits very weak antihistamine and anti-acetylcholine activity on isolated guinea-pig ileum, with initial potentiation of agonist responses during exposure and weak reduction after washout[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Choline theophyllinate (50-200 mg/kg; p.o.; single dose) protects guinea-pigs against acetylcholine-induced bronchospasm with maximum effect at 1 hr and measurable activity persisting for at least 6 hr at higher doses[1].
Choline theophyllinate (10 mg/kg; i.v.) produces a pronounced increase in urine flow in anaesthetized rabbits[1].
Choline theophyllinate (74-337 mg/kg; i.v.; p.o.) has an acute oral LD50 of 337 mg/kg in albino mice and an intravenous LD50 of 74 mg/kg, with an oral-to-intravenous ratio of 4.5 indicating good gastrointestinal absorption[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea-pigs (8 per treatment group)[1]
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Dosage:50 mg/kg (acetylcholine 30% protection, histamine 19% protection); 100 mg/kg (acetylcholine 61% protection, histamine 69% protection)
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Administration:i.p.; single dose 20 min before aerosol challenge
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Result:Provided 30% mean percentage protection against 4% acetylcholine-induced bronchospasm at 50 mg/kg.
Provided 19% mean percentage protection against 2% histamine-induced bronchospasm at 50 mg/kg.
Provided 61% mean percentage protection against 4% acetylcholine-induced bronchospasm at 100 mg/kg.
Provided 69% mean percentage protection against 2% histamine-induced bronchospasm at 100 mg/kg.
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Animal Model:Guinea-pigs (32 total, 4 per time point per compound)[1]
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Dosage:50 mg/kg; 200 mg/kg (activity persists at 6 hr)
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Administration:p.o.; single dose by stomach tube
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Result:Reached maximum protective effect against acetylcholine-induced bronchospasm at 1 hr after oral administration.
Retained some protective effect at 6 hr after dosing at the 200 mg/kg dose.
Chemical Information
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CAS No. 4499-40-5
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Appearance Solid
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Molecular Weight 283.33
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Formula C12H21N5O3
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Color White to off-white
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SMILES
C[N+](C)(CCO)C.CN1C2=C(C(N(C1=O)C)=O)N=C[N-]2
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Synonyms
Oxtriphylline
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
DHRS2 inhibits cell growth and metastasis in ovarian cancer by downregulation of CHKα to disrupt choline metabolism. [Abstract]2022 Oct 3;13(10):845. PMID: 36192391 -
Phytomedicine
Motherwort synergized with oxytocin for postpartum hemorrhage prevention: Integrated clinical efficacy and mechanism exploration. [Abstract]2025 Sep:145:156951. PMID: 40527062 -
J Hazard Mater
EHDPP impairs intestinal microbiota homeostasis and induces placental injury through choline mediated gut-placenta axis. [Abstract]2025 Jun 5:489:137573. PMID: 40007358
Choline theophyllinate purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) demonstrated no cytotoxic effects but partially mitigated the inhibition of cell viability induced by EHDPP in HTR-8/SVneo and JEG-3 cells.
Choline theophyllinate purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) reversed EHDPP-induced cell migration inhibition in HTR-8/SVneo cells.
Choline theophyllinate purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline (30 μM, 24 h) reversed the EHDPP-induced decrease of mRNA levels of TNF-α, IL-6, and IL-1β in HTR-8/SVneo cells.
Choline theophyllinate purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline supplementation (25 mM choline-containing water for 31.5 days) significantly increased uterine size, fetal weight, placental weight, and placental diameter that were reduced by EHDPP exposure.
Choline theophyllinate purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jun 5:489:137573. [Abstract]
Choline supplementation (25 mM choline-containing water for 31.5 days) alleviated the decrease in mRNA expression of the proliferation marker Ki67 and the vascular differentiation marker CD31 induced by EHDPP.
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Antioxidants (Basel)
Role of Mitochondrial Reactive Oxygen Species-Mediated Chaperone-Mediated Autophagy and Lipophagy in Baicalin and N-Acetylcysteine Mitigation of Cadmium-Induced Lipid Accumulation in Liver. [Abstract]2024 Jan 17;13(1):115. PMID: 38247538 -
Solvent & Solubility
In Vitro:
H2O : 250 mg/mL (882.36 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 3.5295 mL | 17.6473 mL | 35.2945 mL | 88.2363 mL |
| 5 mM | 0.7059 mL | 3.5295 mL | 7.0589 mL | 17.6473 mL | |
| 10 mM | 0.3529 mL | 1.7647 mL | 3.5295 mL | 8.8236 mL | |
| 15 mM | 0.2353 mL | 1.1765 mL | 2.3530 mL | 5.8824 mL | |
| 20 mM | 0.1765 mL | 0.8824 mL | 1.7647 mL | 4.4118 mL | |
| 25 mM | 0.1412 mL | 0.7059 mL | 1.4118 mL | 3.5295 mL | |
| 30 mM | 0.1176 mL | 0.5882 mL | 1.1765 mL | 2.9412 mL | |
| 40 mM | 0.0882 mL | 0.4412 mL | 0.8824 mL | 2.2059 mL | |
| 50 mM | 0.0706 mL | 0.3529 mL | 0.7059 mL | 1.7647 mL | |
| 60 mM | 0.0588 mL | 0.2941 mL | 0.5882 mL | 1.4706 mL | |
| 80 mM | 0.0441 mL | 0.2206 mL | 0.4412 mL | 1.1030 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3529 mL | 0.8824 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Choline theophyllinate Related Classifications
HY-B1718 Related Classifications
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