2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Apoptosis
  4. 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.

Tofacitinib Prodrug-1 Chemical Structure

Tofacitinib Prodrug-1 Chemical Structure

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Tofacitinib Prodrug-1 Related Antibodies

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Description

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[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].

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

Tofacitinib Prodrug-1 Related Antibodies
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].

MedChemExpress (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
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tofacitinib Prodrug-1 Related Classifications

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  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tofacitinib Prodrug-1Tofacitinib Prodrug1Tofacitinib Prodrug 1JAKApoptosisJanus kinaseTofacitinibProdrugUlcerative colitisInflammationSystemic adverse effectsOralInhibitorinhibitorinhibit

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