|11R-VIVIT游离态|CsnPharm

CAS No.: 249537-73-3

NFAT Inhibitor-1/11R-VIVIT游离态 Catalog No. CSN23754

Synonyms: VIVIT peptide;Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu;11R-VIVIT

NFAT Inhibitor is a high-affinity calcineurin-binding peptide that inhibits NFAT (Nuclear Factor of Activated T cells) activation and NFAT-dependent expression of endogenous cytokine genes in T cells.

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技术信息

生物活性

描述The nuclear factor of activated T cells (NFAT) is a family of transcription factors that regulate immune responses and adaptive response in skeletal and cardiac muscle. NFAT inhibitor (VIVIT peptide) is a cell-permeable peptide that selectively inhibits calcineurin-mediated dephosphorylation of NFAT^[1]. In peripheral blood CD14+ monocytes isolated from rheumatoid arthritis patients, treatment with 10μM of NFAT inhibitor plus 100ng/mL of recombinant human RANKL and 50ng/mL of M‐CSF for 24h significantly inhibited nuclear translocation of NFATc1, but not that of peroxisome proliferator-activated receptor γ coactivator 1β. Long-term (21 days) treatment with NFAT inhibitor in combination with M‐CSF and RANKL significantly inhibited the cytoplasmic levels of cathepsin K, tartrate‐resistant acid phosphatase, and matrix metalloproteinase 9^[2]. Intraperitoneal administration of NFAT (10mg/kg) once daily for 2 days prevented T-cell activation and proliferation in C3H/HeN mice^[3].
作用机制NFAT inhibitor potently and selectively inhibits the NFAT-calcineurin interaction without affecting calcineurin phosphatase activity. It was developed based on the conserved calcineurin docking site of NFAT^[1].
参考文献

[1] Aramburu J, Yaffe MB, López-Rodríguez C, Cantley LC, Hogan PG, Rao A. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999;285(5436):2129-2133. doi:10.1126/science.285.5436.2129
[2] Ma JD, Jing J, Wang JW, et al. Activation of the Peroxisome Proliferator-Activated Receptor γ Coactivator 1β/NFATc1 Pathway in Circulating Osteoclast Precursors Associated With Bone Destruction in Rheumatoid Arthritis. Arthritis Rheumatol. 2019;71(8):1252-1264. doi:10.1002/art.40868
[3] Noguchi H, Matsushita M, Okitsu T, et al. A new cell-permeable peptide allows successful allogeneic islet transplantation in mice. Nat Med. 2004;10(3):305-309.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.5938 mL
- 2.9692 mL
- 5.9385 mL
- 5 mM
- 0.1188 mL
- 0.5938 mL
- 1.1877 mL
- 10 mM
- 0.0594 mL
- 0.2969 mL
- 0.5938 mL

技术信息

CAS号

249537-73-3

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C75H120N20O22S

运输

蓝冰

分子量

1685.94

别名

VIVIT peptide;Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu;11R-VIVIT;NFAT Inhibitor

溶解度

Water

100.0 mg/mL (59.3 mM) warming

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NFAT Inhibitor-1/11R-VIVIT游离态 Catalog No. CSN23754

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