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manitimus

CAS No.:
202057-76-9
Catalog Number:
AG00BHVG
Molecular Formula:
C15H11F3N2O2
Molecular Weight:
308.2552
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
1mg
99%
1 week
United States
$390
- +
5mg
99%
1 week
United States
$723
- +
10mg
99%
1 week
United States
$1190
- +
20mg
99%
1 week
United States
$2057
- +
Product Description
Catalog Number:
AG00BHVG
Chemical Name:
manitimus
CAS Number:
202057-76-9
Molecular Formula:
C15H11F3N2O2
Molecular Weight:
308.2552
MDL Number:
MFCD00922017
IUPAC Name:
(Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]hept-2-en-6-ynamide
InChI:
InChI=1S/C15H11F3N2O2/c1-2-3-4-13(21)12(9-19)14(22)20-11-7-5-10(6-8-11)15(16,17)18/h1,5-8,21H,3-4H2,(H,20,22)/b13-12-
InChI Key:
IRELROQHIPLASX-SEYXRHQNSA-N
SMILES:
N#C/C(=C(\CCC#C)/O)/C(=O)Nc1ccc(cc1)C(F)(F)F
UNII:
4B135RK2KL
Properties
Complexity:
540  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
1  
Exact Mass:
308.077g/mol
Formal Charge:
0
Heavy Atom Count:
22  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
2  
Isotope Atom Count:
0
Molecular Weight:
308.26g/mol
Monoisotopic Mass:
308.077g/mol
Rotatable Bond Count:
4  
Topological Polar Surface Area:
73.1A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
3.7  
Literature
Title Journal
The inhibitors of nucleotide biosynthesis leflunomide, FK778, and mycophenolic acid activate hepatitis B virus replication in vitro. Hepatology (Baltimore, Md.) 20120701
A multicenter, randomized, double-blind study comparing different FK778 doses (manitimus) with tacrolimus and steroids vs. MMF with tacrolimus and steroids in renal transplantation. BMC nephrology 20120101
Assessment of efficacy and safety of FK778 in comparison with standard care in renal transplant recipients with untreated BK nephropathy. Transplantation 20101027
Leflunomide derivate FK 778 in accelerated renal injury in transgenic rat. Folia biologica 20100101
Leflunomide derivative FK778 inhibits production of antibodies in an experimental model of alloreactive T-B cell interaction. Experimental and clinical transplantation : official journal of the Middle East Society for Organ Transplantation 20091201
The effect of Malononitrilamides (FK778) on phenotypic properties of human peripheral dendritic cells. Transplantation proceedings 20090601
Cellular growth inhibition by FK778 is linked to G1 arrest or S phase accumulation, dependent on the functional status of the retinoblastoma protein. International journal of molecular medicine 20090301
The new immunosuppressive agent FK778 attenuates neointima formation in an experimental venous bypass graft model. Vascular pharmacology 20090101
FK778 attenuates cytomegalovirus-enhanced vein graft intimal hyperplasia in a rat model. Intervirology 20090101
FK778 ameliorates post-transplant expression of fibrogenic growth factors and development of chronic rejection changes in rat kidney allografts. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association 20081101
Prevention and inhibition but not reversion of chronic allograft vasculopathy by FK778. Transplantation 20080327
The new malononitrilamide immunosuppressant FK778 prolongs corneal allograft survival in the rat keratoplasty model. Eye (London, England) 20071201
The effect of FK778 on the progression of chronic allograft nephropathy in a rat model. Transplantation 20070327
Is the malononitrilamide FK778 better for the prevention of acute or chronic rejection? Transplantation proceedings 20070301
The immunosuppressive drug FK778 induces regulatory activity in stimulated human CD4+ CD25- T cells. Blood 20070101
Inhibition of restenosis development after mechanical injury: a new field of application for malononitrilamides? Cardiology 20070101
Impairment of T cell interactions with antigen-presenting cells by immunosuppressive drugs reveals involvement of calcineurin and NF-kappaB in immunological synapse formation. Journal of leukocyte biology 20070101
FK778 in experimental xenotransplantation: a detailed analysis of drug efficacy. The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation 20070101
Prolonged survival with FK778 (malononitrilamide) monotherapy after small bowel transplantation: a large animal study. Transplantation proceedings 20070101
The effect of leflunomide analogue FK778 on development of chronic rat renal allograft rejection and transforming growth factor-BETA expression. Transplantation proceedings 20061201
The effect of FK778 on acute rat renal allograft rejection and expression of platelet-derived growth factor and transforming growth factor-beta. Transplantation proceedings 20061001
Sirolimus and FK778: a comparison of two anti-proliferative immunosuppressants for prevention of experimental obliterative airway disease. Transplant international : official journal of the European Society for Organ Transplantation 20060401
FK778: new cellular and molecular mechanisms of action. Transplantation proceedings 20060401
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. International journal of immunopathology and pharmacology 20060101
FK778 does not impair intestinal allograft absorption in a preclinical model of total small bowel transplantation. Transplantation proceedings 20060101
FK778 and tacrolimus combination therapy to control acute rejection after pig intestinal transplantation. Transplantation proceedings 20060101
FK778 and tacrolimus prevent the development of obliterative airway disease after heterotopic rat tracheal transplantation. The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation 20051101
Inhibition of human dendritic cell maturation and function by the novel immunosuppressant FK778. Transplantation 20051027
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 of vascular and interventional radiology : JVIR 20050701
FK-778 Astellas. Current opinion in investigational drugs (London, England : 2000) 20050501
The novel immunosuppressant FK778 inhibits formation of the immunologic Synapse. Transplantation proceedings 20050501
Mechanistic study of malononitrileamide FK778 in cardiac transplantation and CMV infection in rats. Transplantation 20050115
Inhibition of human cytomegalovirus signaling and replication by the immunosuppressant FK778. Antiviral research 20050101
FK778 controls acute rejection after rat liver allotransplantation showing positive interaction with FK506. Transplantation proceedings 20050101
In vivo metabolism for the hydroxylation of FK778 to the metabolite M3 in humans studied by enantioselective liquid chromatography/tandem mass spectrometry. Rapid communications in mass spectrometry : RCM 20050101
Efficacy of malononitrilamide FK778 in a preclinical model of small bowel transplantation. Transplantation proceedings 20050101
Assessment of an LC-MS method for plasma quantification of the new immunosuppressant FK778 through comparison with HPLC-UV. Transplantation proceedings 20050101
FK778, a synthetic malononitrilamide. Yonsei medical journal 20041231
FK778 and FK506 combination therapy to control acute rejection after rat liver allotransplantation. Transplantation 20041215
FK778: a powerful immunosuppressive, but will it really be good for you? Transplantation 20040715
The effects of FK778 in combination with tacrolimus and steroids: a phase II multicenter study in renal transplant patients. Transplantation 20040715
FK778 attenuates lymphocyte-endothelium interaction after cardiac transplantation: in vivo and in vitro studies. Transplantation 20040715
New drugs to improve transplant outcomes. Transplantation 20040515
The interaction between FK778 and tacrolimus in the prevention of rat cardiac allograft rejection is dose dependent. Transplantation 20040227
New immunosuppressive strategies in renal transplant recipients. Journal of nephrology 20040101
Immunosuppression with FK778 and mycophenolate mofetil in a rat cardiac transplantation model. Transplantation 20031215
Leflunomide analogue FK778 is vasculoprotective independent of its immunosuppressive effect: potential applications for restenosis and chronic rejection. Transplantation 20030815
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. Transplantation 20030615
Combination therapy of malononitrilamide FK778 with tacrolimus on cell proliferation assays and in rats receiving renal allografts. Transplantation 20030515
In vivo pharmacokinetic and pharmacodynamic evaluation of the malononitrilamide FK778 in non-human primates. Transplant international : official journal of the European Society for Organ Transplantation 20030501
FK778, a powerful new immunosuppressant, effectively reduces functional and histologic changes of chronic rejection in rat renal allografts. Transplantation 20030427
Significant prolongation of renal allograft survival by delayed combination therapy of FK778 with tacrolimus in nonhuman primates. Transplantation 20030427
Immunosuppression with a combination of the leflunomide analog, FK778, and microemulsified cyclosporine for renal transplantation in mongrel dogs. Transplantation 20030427
Modified noble plication for the prevention of intestinal intussusception after renal transplantation in dogs. Journal of investigative surgery : the official journal of the Academy of Surgical Research 20030101
Effects of the malononitrilamide FK778 on immune functions in vitro in whole blood from non-human primates and healthy human volunteers. Transplant immunology 20030101
A novel leflunomide derivative, FK778, for immunosuppression after kidney transplantation in dogs. Surgery 20020701
An evaluation of combined immunosuppression with MNA 715 and microemulsified cyclosporine on renal allograft rejection in mismatched mongrel dogs. Veterinary surgery : VS 20020101
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. Transplantation proceedings 20010501
Efficacy of malononitrilamide 715 as immunosuppressant, alone or in combination with cyclosporin, in allogeneic foetal rat pancreatic transplantation. Transplantation proceedings 20010501
Development of a novel drug for transplantation: current results and future perspectives. Transplantation proceedings 20010501
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? European journal of biochemistry 20010301
Leflunomide analog, MNA-715, plus cyclosporine reduces renal allograft rejection in mismatched dogs. Transplantation proceedings 20010101
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives. Biochemical pharmacology 19981101
Structural and functional comparison of agents interfering with dihydroorotate, succinate and NADH oxidation of rat liver mitochondria. Biochemical pharmacology 19981015
Properties