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

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Tofacitinib Prodrug-1 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Tofacitinib Prodrug-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tofacitinib Prodrug-1
Cat. No.:
HY-145829
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.