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  3. Tofacitinib Prodrug-1

Tofacitinib Prodrug-1 

Cat. No.: HY-145829
Handling Instructions

Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib Prodrug-1 is a potential drug candidate for the treatment of ulcerative colitis.

For research use only. We do not sell to patients.

Tofacitinib Prodrug-1 Chemical Structure

Tofacitinib Prodrug-1 Chemical Structure

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Description

Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib Prodrug-1 is a potential drug candidate for the treatment of ulcerative colitis[1].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tofacitinib Prodrug-1 (22.5 mg/kg; p.o.) can decrease the systemic exposure of tofacitinib by releasing the parent drug Tofacitinib into the circulation slowly[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rats (5-6 weeks, 220-250 g, n=6) (pharmacokinetic)[1]
Dosage: 22.5 mg/kg
Administration: p.o.; blood were taken at 1, 2, 4, 6, 8, 12, 14, and 20 hours
Result: Decreased the systemic exposure of tofacitinib by releasing the parent drug tofacitinib into the circulation slowly.
Animal Model: Male BALB/c mice (5-6 weeks, 25-30 g, n = 6)[1]
Dosage: 22.5 mg/kg
Administration: p.o.; blood and intestinal tissues were taken at 0.5, 1, 2, 3, 4, 6, 9, and 12 hours
Result: Increased intestinal exposure to improve the therapeutic effect of tofacitinib.
Animal Model: Male BALB/c mice (5-6 weeks, 25-28 g, n=7-9)[1]
Dosage: 1.5 mg/kg
Administration: p.o.; twice daily, for 4 days
Result: Tofacitinib Prodrug-1 could effectively attenuate the oxazolone-induced colitis in mice.
Animal Model: Male BALB/c mice (5-6 weeks, 25-28 g, n = 10)[1]
Dosage: 1.5 mg/kg
Administration: i.g.; twice daily, for 4 days
Result: Had no apparent influence on systemic immunosuppression in normal mice, which could decrease the risk of infection associated with tofacitinib.
Animal Model: Kunming mice (18-22 g; n = 10)[1]
Dosage: 2000 mg/kg
Administration: i.g.; single
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.
Molecular Weight

759.21

Formula

C36H39ClN10O7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Tofacitinib Prodrug-1
Cat. No.:
HY-145829
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