Tofacitinib Prodrug-1
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis.
For research use only. We do not sell to patients.
- Formula: C36H39ClN10O7
- Molecular Weight:759.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Tofacitinib Prodrug-1 (compound 20g) (1 mM; 12 hours at 37 °C) is not obviously degraded from 0 to 12 hours in simulated gastric and intestinal fluid[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tofacitinib Prodrug-1 (22.5 mg/kg; p.o.) can increase intestinal exposure to improve the therapeutic effect of Tofacitinib[1].
Tofacitinib Prodrug-1 (1.5 mg/kg; p.o.; twice daily, for 4 days) can effectively attenuate the oxazolone-induced colitis in mice[1].
Tofacitinib Prodrug-1 (1.5 mg/kg; i.g.; twice daily, for 4 days) has no apparent influence on systemic immunosuppression in normal mice, which could decrease the risk of infection associated with Tofacitinib[1].
Tofacitinib Prodrug-1 (2000 mg/kg; i.g.; single) has low toxicity and was tolerated at an oral dose of 2000 mg/kg, and no significant change was observed in biochemical parameters and organ indexes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rats (5-6 weeks, 220-250 g, n=6) (pharmacokinetic)[1]
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Dosage:22.5 mg/kg
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Administration:p.o.; blood were taken at 1, 2, 4, 6, 8, 12, 14, and 20 hours
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Result:Decreased the systemic exposure of tofacitinib by releasing the parent drug tofacitinib into the circulation slowly.
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Animal Model:Male BALB/c mice (5-6 weeks, 25-30 g, n = 6)[1]
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Dosage:22.5 mg/kg
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Administration:p.o.; blood and intestinal tissues were taken at 0.5, 1, 2, 3, 4, 6, 9, and 12 hours
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Result:Increased intestinal exposure to improve the therapeutic effect of tofacitinib.
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Animal Model:Male BALB/c mice (5-6 weeks, 25-28 g, n=7-9)[1]
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Dosage:1.5 mg/kg
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Administration:p.o.; twice daily, for 4 days
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Result:Tofacitinib Prodrug-1 could effectively attenuate the oxazolone-induced colitis in mice.
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Animal Model:Male BALB/c mice (5-6 weeks, 25-28 g, n = 10)[1]
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Dosage:1.5 mg/kg
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Administration:i.g.; twice daily, for 4 days
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Result:Had no apparent influence on systemic immunosuppression in normal mice, which could decrease the risk of infection associated with tofacitinib.
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Animal Model:Kunming mice (18-22 g; n = 10)[1]
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Dosage:2000 mg/kg
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Administration:i.g.; single
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Result:Had low toxicity and was tolerated at an oral dose of 2000 mg/kg, and no significant change was observed in biochemical parameters and organ indexes.
Chemical Information
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Molecular Weight 759.21
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Formula C36H39ClN10O7
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SMILES
O=C(O)C1=CC(/N=N/C2=CC=C(COC(NCCCN(C)C(N3C=CC4=C(NC[C@@H]5CN(C(CC#N)=O)CC[C@H]5C)N=CN=C43)=O)=O)C(Cl)=C2)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tofacitinib Prodrug-1 Related Classifications
HY-145829 Related Classifications
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