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202057-76-9,MFCD00922017
Catalog No.:AA00BHSO

202057-76-9 | manitimus

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1mg
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$431.00   $302.00
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5mg
99%
1 week  
$812.00   $569.00
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10mg
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$1,346.00   $942.00
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20mg
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  • Technical Information
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00BHSO
Chemical Name:
manitimus
CAS Number:
202057-76-9
Molecular Formula:
C15H11F3N2O2
Molecular Weight:
308.2552
MDL Number:
MFCD00922017
SMILES:
N#C/C(=C(\CCC#C)/O)/C(=O)Nc1ccc(cc1)C(F)(F)F
Properties
Computed Properties
 
Complexity:
540  
Covalently-Bonded Unit Count:
1  
Defined Bond Stereocenter Count:
1  
Heavy Atom Count:
22  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
4  
XLogP3:
3.7  

Literature

Title: The inhibitors of nucleotide biosynthesis leflunomide, FK778, and mycophenolic acid activate hepatitis B virus replication in vitro.

Journal: Hepatology (Baltimore, Md.) 20120701

Title: A multicenter, randomized, double-blind study comparing different FK778 doses (manitimus) with tacrolimus and steroids vs. MMF with tacrolimus and steroids in renal transplantation.

Journal: BMC nephrology 20120101

Title: Assessment of efficacy and safety of FK778 in comparison with standard care in renal transplant recipients with untreated BK nephropathy.

Journal: Transplantation 20101027

Title: Leflunomide derivate FK 778 in accelerated renal injury in transgenic rat.

Journal: Folia biologica 20100101

Title: Leflunomide derivative FK778 inhibits production of antibodies in an experimental model of alloreactive T-B cell interaction.

Journal: Experimental and clinical transplantation : official journal of the Middle East Society for Organ Transplantation 20091201

Title: The effect of Malononitrilamides (FK778) on phenotypic properties of human peripheral dendritic cells.

Journal: Transplantation proceedings 20090601

Title: Cellular growth inhibition by FK778 is linked to G1 arrest or S phase accumulation, dependent on the functional status of the retinoblastoma protein.

Journal: International journal of molecular medicine 20090301

Title: The new immunosuppressive agent FK778 attenuates neointima formation in an experimental venous bypass graft model.

Journal: Vascular pharmacology 20090101

Title: FK778 attenuates cytomegalovirus-enhanced vein graft intimal hyperplasia in a rat model.

Journal: Intervirology 20090101

Title: FK778 ameliorates post-transplant expression of fibrogenic growth factors and development of chronic rejection changes in rat kidney allografts.

Journal: Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20081101

Title: Prevention and inhibition but not reversion of chronic allograft vasculopathy by FK778.

Journal: Transplantation 20080327

Title: The new malononitrilamide immunosuppressant FK778 prolongs corneal allograft survival in the rat keratoplasty model.

Journal: Eye (London, England) 20071201

Title: The effect of FK778 on the progression of chronic allograft nephropathy in a rat model.

Journal: Transplantation 20070327

Title: Is the malononitrilamide FK778 better for the prevention of acute or chronic rejection?

Journal: Transplantation proceedings 20070301

Title: The immunosuppressive drug FK778 induces regulatory activity in stimulated human CD4+ CD25- T cells.

Journal: Blood 20070101

Title: Inhibition of restenosis development after mechanical injury: a new field of application for malononitrilamides?

Journal: Cardiology 20070101

Title: Impairment of T cell interactions with antigen-presenting cells by immunosuppressive drugs reveals involvement of calcineurin and NF-kappaB in immunological synapse formation.

Journal: Journal of leukocyte biology 20070101

Title: FK778 in experimental xenotransplantation: a detailed analysis of drug efficacy.

Journal: The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation 20070101

Title: Prolonged survival with FK778 (malononitrilamide) monotherapy after small bowel transplantation: a large animal study.

Journal: Transplantation proceedings 20070101

Title: The effect of leflunomide analogue FK778 on development of chronic rat renal allograft rejection and transforming growth factor-BETA expression.

Journal: Transplantation proceedings 20061201

Title: The effect of FK778 on acute rat renal allograft rejection and expression of platelet-derived growth factor and transforming growth factor-beta.

Journal: Transplantation proceedings 20061001

Title: Sirolimus and FK778: a comparison of two anti-proliferative immunosuppressants for prevention of experimental obliterative airway disease.

Journal: Transplant international : official journal of the European Society for Organ Transplantation 20060401

Title: FK778: new cellular and molecular mechanisms of action.

Journal: Transplantation proceedings 20060401

Title: Role of FK778 alone or in combination with tacrolimus or mTOR inhibitors as an immunomodulator of immunofunctions: in vitro evaluation of T cell proliferation and the expression of lymphocyte surface antigens.

Journal: International journal of immunopathology and pharmacology 20060101

Title: FK778 does not impair intestinal allograft absorption in a preclinical model of total small bowel transplantation.

Journal: Transplantation proceedings 20060101

Title: FK778 and tacrolimus combination therapy to control acute rejection after pig intestinal transplantation.

Journal: Transplantation proceedings 20060101

Title: FK778 and tacrolimus prevent the development of obliterative airway disease after heterotopic rat tracheal transplantation.

Journal: The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation 20051101

Title: Inhibition of human dendritic cell maturation and function by the novel immunosuppressant FK778.

Journal: Transplantation 20051027

Title: 2005 Dr. Gary J. Becker Young Investigator Award: periprocedural oral administration of the leflunomide analogue FK778 inhibits neointima formation in a double-injury rat model of restenosis.

Journal: Journal of vascular and interventional radiology : JVIR 20050701

Title: FK-778 Astellas.

Journal: Current opinion in investigational drugs (London, England : 2000) 20050501

Title: The novel immunosuppressant FK778 inhibits formation of the immunologic Synapse.

Journal: Transplantation proceedings 20050501

Title: Mechanistic study of malononitrileamide FK778 in cardiac transplantation and CMV infection in rats.

Journal: Transplantation 20050115

Title: Inhibition of human cytomegalovirus signaling and replication by the immunosuppressant FK778.

Journal: Antiviral research 20050101

Title: FK778 controls acute rejection after rat liver allotransplantation showing positive interaction with FK506.

Journal: Transplantation proceedings 20050101

Title: In vivo metabolism for the hydroxylation of FK778 to the metabolite M3 in humans studied by enantioselective liquid chromatography/tandem mass spectrometry.

Journal: Rapid communications in mass spectrometry : RCM 20050101

Title: Efficacy of malononitrilamide FK778 in a preclinical model of small bowel transplantation.

Journal: Transplantation proceedings 20050101

Title: Assessment of an LC-MS method for plasma quantification of the new immunosuppressant FK778 through comparison with HPLC-UV.

Journal: Transplantation proceedings 20050101

Title: FK778, a synthetic malononitrilamide.

Journal: Yonsei medical journal 20041231

Title: FK778 and FK506 combination therapy to control acute rejection after rat liver allotransplantation.

Journal: Transplantation 20041215

Title: FK778: a powerful immunosuppressive, but will it really be good for you?

Journal: Transplantation 20040715

Title: The effects of FK778 in combination with tacrolimus and steroids: a phase II multicenter study in renal transplant patients.

Journal: Transplantation 20040715

Title: FK778 attenuates lymphocyte-endothelium interaction after cardiac transplantation: in vivo and in vitro studies.

Journal: Transplantation 20040715

Title: New drugs to improve transplant outcomes.

Journal: Transplantation 20040515

Title: The interaction between FK778 and tacrolimus in the prevention of rat cardiac allograft rejection is dose dependent.

Journal: Transplantation 20040227

Title: New immunosuppressive strategies in renal transplant recipients.

Journal: Journal of nephrology 20040101

Title: Immunosuppression with FK778 and mycophenolate mofetil in a rat cardiac transplantation model.

Journal: Transplantation 20031215

Title: Leflunomide analogue FK778 is vasculoprotective independent of its immunosuppressive effect: potential applications for restenosis and chronic rejection.

Journal: Transplantation 20030815

Title: Synergistic effects of malononitrilamides (FK778, FK779) with tacrolimus (FK506) in prevention of acute heart and kidney allograft rejection and reversal of ongoing heart allograft rejection in the rat.

Journal: Transplantation 20030615

Title: Combination therapy of malononitrilamide FK778 with tacrolimus on cell proliferation assays and in rats receiving renal allografts.

Journal: Transplantation 20030515

Title: In vivo pharmacokinetic and pharmacodynamic evaluation of the malononitrilamide FK778 in non-human primates.

Journal: Transplant international : official journal of the European Society for Organ Transplantation 20030501

Title: FK778, a powerful new immunosuppressant, effectively reduces functional and histologic changes of chronic rejection in rat renal allografts.

Journal: Transplantation 20030427

Title: Significant prolongation of renal allograft survival by delayed combination therapy of FK778 with tacrolimus in nonhuman primates.

Journal: Transplantation 20030427

Title: Immunosuppression with a combination of the leflunomide analog, FK778, and microemulsified cyclosporine for renal transplantation in mongrel dogs.

Journal: Transplantation 20030427

Title: Modified noble plication for the prevention of intestinal intussusception after renal transplantation in dogs.

Journal: Journal of investigative surgery : the official journal of the Academy of Surgical Research 20030101

Title: Effects of the malononitrilamide FK778 on immune functions in vitro in whole blood from non-human primates and healthy human volunteers.

Journal: Transplant immunology 20030101

Title: A novel leflunomide derivative, FK778, for immunosuppression after kidney transplantation in dogs.

Journal: Surgery 20020701

Title: An evaluation of combined immunosuppression with MNA 715 and microemulsified cyclosporine on renal allograft rejection in mismatched mongrel dogs.

Journal: Veterinary surgery : VS 20020101

Title: Leflunomide and its analogue X920715 synergize with cyclosporin A in preventing early graft failure and delaying graft rejection of xenogeneic islets in nonobese diabetic mice.

Journal: Transplantation proceedings 20010501

Title: Efficacy of malononitrilamide 715 as immunosuppressant, alone or in combination with cyclosporin, in allogeneic foetal rat pancreatic transplantation.

Journal: Transplantation proceedings 20010501

Title: Development of a novel drug for transplantation: current results and future perspectives.

Journal: Transplantation proceedings 20010501

Title: Recombinant expression of N-terminal truncated mutants of the membrane bound mouse, rat and human flavoenzyme dihydroorotate dehydrogenase. A versatile tool to rate inhibitor effects?

Journal: European journal of biochemistry 20010301

Title: Leflunomide analog, MNA-715, plus cyclosporine reduces renal allograft rejection in mismatched dogs.

Journal: Transplantation proceedings 20010101

Title: Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives.

Journal: Biochemical pharmacology 19981101

Title: Structural and functional comparison of agents interfering with dihydroorotate, succinate and NADH oxidation of rat liver mitochondria.

Journal: Biochemical pharmacology 19981015

Title: Birnbaum F, et al. The new malononitrilamide immunosuppressant FK778 prolongs corneal allograft survival in the rat keratoplasty model. Eye (Lond). 2007 Dec;21(12):1516-23. Epub 2007 Mar 30.

Title: Kloppenburg G, et al. FK778 attenuates cytomegalovirus-enhanced vein graft intimal hyperplasia in a rat model. Intervirology. 2009;52(4):189-95.

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