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Chemical Structure| 249537-73-3 Chemical Structure| 249537-73-3

Structure of NFAT Inhibitor-1
CAS No.: 249537-73-3

Chemical Structure| 249537-73-3

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The NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide that selectively inhibits the calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT).

Synonyms: VIVIT peptide; NFAT Inhibitor

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Product Details of NFAT Inhibitor-1

CAS No. :249537-73-3
Formula : C75H120N20O22S
M.W : 1685.94
SMILES Code : O=C([C@H]1N(CCC1)C(CNC([C@H](C)NC([C@@H](N)CCSC)=O)=O)=O)N[C@@H](CC2=CNC=N2)C(N(CC)[C@@H](C)C(N[C@@H](C(C)C)C(N[C@]([C@@H](C)CC)([H])C(N[C@@H](C(C)C)C(N[C@]([C@@H](C)CC)([H])C(N[C@]([C@H](O)C)([H])C(NCC(N3[C@@H](CCC3)C(N[C@H](C(N[C@@H](CCC(O)=O)C(N[C@H](C(O)=O)CCC(O)=O)=O)=O)CC4=CNC=N4)=O)=O)=O)=O)=O)=O)=O)=O)=O
Synonyms :
VIVIT peptide; NFAT Inhibitor
MDL No. :MFCD02683959
InChI Key :QPMHUXBSHGAVGD-MCDIZDEASA-N
Pubchem ID :16135717

Safety of NFAT Inhibitor-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMMs) 5 μM 1 hour Inhibited LPS-induced expression of TNF, MIP-1α and IL-1β PMC3169434
LN229 cells 500 µM 24 h and 48 h To evaluate the effect of Sim2-VIVIT on NFAT signaling, results showed Sim2-VIVIT did not affect the pattern of NFATc1 bands or NFAT-dependent promoter activity PMC8400789
Primary murine microglia 10 μM 24 hours To assess the effect of NFAT inhibitors on cytokine and neurotoxin secretion by Aβ-stimulated microglia. Results showed that tat-VIVIT and FK506 significantly attenuated Aβ- and LPS-stimulated secretion of TNFα and IL-6. PMC4355356
U87 cells 20 µM 25 h To evaluate the effect of 11R-VIVIT on NFAT activity, results showed 11R-VIVIT at 20 µM upregulated NFAT-dependent promoter activity, but the increase was not statistically significant PMC8400789
LN229 cells 20 µM 25 h To evaluate the effect of 11R-VIVIT on NFAT activity, results showed 11R-VIVIT at 10 µM and 20 µM activated NFAT-dependent promoter activity PMC8400789
ARPE-19 cells 10 µM 4 hours pretreatment followed by 24 hours LPS treatment To evaluate the effect of VIVIT on LPS-induced NFAT luciferase activity, results showed that VIVIT significantly reduced LPS-induced luciferase activity. PMC8395439
Bone marrow macrophages 1 μM 48 hours Inhibited NFATc1 expression and significantly downregulated Nod1 mRNA expression PMC3561241
HPV E6/E7 immortalized mouse RPE cells 20 µM 48 hours To study the effect of VIVIT on starvation-induced TFEB nuclear localization, results showed that VIVIT caused TFEB retention in the cytoplasm. PMC8395439
ARPE-19 cells 20 µM 48 hours To investigate the effect of NFAT inhibition on TFEB expression, results showed that VIVIT treatment did not significantly alter TFEB expression levels. PMC8395439
Mouse bone marrow macrophages (BMMs) 2.0 μM 96 hours To investigate the effect of VIVIT peptide on wear particle-induced osteoclastogenesis from BMMs. Results showed that VIVIT significantly inhibited wear particle (Ti and PMMA)-induced osteoclast formation and bone resorption activity. PMC4006473

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
APP/PS1 transgenic mice Alzheimer's disease model Subcutaneous injection 0.5 mg/kg/day Continuous for 28 days To evaluate the effect of NFAT inhibitors on microglial activation, Aβ plaque load, and memory in APP/PS1 mice. Results showed that FK506 and tat-VIVIT significantly attenuated microgliosis and Aβ plaque load but did not significantly affect memory performance. PMC4355356
Mice Renal retrograde infection model Intraperitoneal injection 10 mg/kg Once daily for 48 hours 11R-VIVIT significantly impaired neutrophil bacterial phagocytic killing capacity and increased renal susceptibility to UPEC PMC3561241
Mice Aortic banding (AB)-induced cardiac hypertrophy model Subcutaneous injection 10 mg/kg Every 2 days for 4 weeks Inhibition of NFAT activity, alleviating the aggravated cardiac hypertrophy pathology caused by Nulp1 deficiency PMC7660797
Mice Aortic banding (AB)-induced cardiac hypertrophy model Subcutaneous osmotic pump 10 mg/kg/day Once daily for 2 weeks Pre-treatment with VIVIT significantly attenuated AB-induced cardiac remodeling abnormalities in IRF8/C0//C0 mice, as evidenced by reduced ratios of HW/BW, LW/BW and HW/TL, and decreased cardiomyocyte cross-sectional area and collagen volume. PMC3929801
APP/PS1 transgenic mice Alzheimer's disease model Stereotactic intracortical injection 2 × 10^12 μg/ml Single injection, observed for 1 month Overexpression of VIVIT-GFP or NLS-VIVIT-GFP significantly improves the decreased spine density and neuritic abnormalities observed near amyloid plaques in APP/PS1 mice, partially restoring neuritic morphological parameters. PMC3296329
Rat Regenerating and adult rat muscles Intramuscular injection 50 μg 7 days The VIVIT peptide blocked Cn-mediated NFAT activation, inhibited the expression of slow myosin heavy chain (MyHC-slow), and upregulated the expression of fast myosin heavy chains (MyHC-2X and MyHC-2B). PMC489979

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.59mL

0.12mL

0.06mL

2.97mL

0.59mL

0.30mL

5.94mL

1.19mL

0.59mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

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