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NFAT Inhibitor

Cat No.:V31220 Purity: ≥98%
NFAT Inhibitor (VIVIT peptide) is a cell-penetrating/penetrable peptide inhibitor of NFAT that selectively inhibits calcineurin-mediated NFAT dephosphorylation.
NFAT Inhibitor
NFAT Inhibitor Chemical Structure CAS No.: 249537-73-3
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
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Product Description
NFAT Inhibitor (VIVIT peptide) is a cell-penetrating/penetrable peptide inhibitor of NFAT that selectively inhibits calcineurin-mediated NFAT dephosphorylation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
For a whole day, NFAT Inhibitor-1 therapy dramatically reduced NFATc1's nuclear translocation. The levels of cathepsin K, TRAP, and MMP-9 in the cytoplasm are markedly inhibited by long-term VIVIT therapy [2].
Cell Assay
Western Blot analysis [2]
Cell Types: Human peripheral blood CD14+ monocytes
Tested Concentrations: 10 μM
Incubation Duration: 24 hrs (hours) or 21 days
Experimental Results: Short-term treatment with 10 μM Dramatically inhibited the nuclear translocation of NFATc1. Long-term treatment Dramatically inhibited the levels of cytoplasmic cathepsin K, TRAP and MMP-9.
References

[1]. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999 Sep 24;285(5436):2129-33.

[2]. 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 Aug;71(8):1252-1264.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C75H118N20O22S
Molecular Weight
1683.92523622513
Exact Mass
1682.845
CAS #
249537-73-3
PubChem CID
16135717
Appearance
White to off-white solid powder
Density
1.3±0.1 g/cm3
Boiling Point
1982.4±65.0 °C at 760 mmHg
Flash Point
1152.7±34.3 °C
Vapour Pressure
0.0±0.3 mmHg at 25°C
Index of Refraction
1.580
LogP
-0.76
Hydrogen Bond Donor Count
19
Hydrogen Bond Acceptor Count
26
Rotatable Bond Count
48
Heavy Atom Count
118
Complexity
3550
Defined Atom Stereocenter Count
17
SMILES
CC[C@H](C)[C@@H](C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CN=CN2)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CC4=CN=CN4)NC(=O)[C@@H]5CCCN5C(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CCSC)N
InChi Key
QPMHUXBSHGAVGD-MCDIZDEASA-N
InChi Code
InChI=1S/C75H118N20O22S/c1-12-39(7)59(90-70(111)57(37(3)4)88-68(109)52-19-16-27-95(52)74(115)49(30-44-32-78-36-82-44)87-67(108)51-18-15-26-94(51)53(97)33-79-62(103)41(9)83-63(104)45(76)24-28-118-11)72(113)89-58(38(5)6)71(112)91-60(40(8)13-2)73(114)92-61(42(10)96)69(110)80-34-54(98)93-25-14-17-50(93)66(107)86-48(29-43-31-77-35-81-43)65(106)84-46(20-22-55(99)100)64(105)85-47(75(116)117)21-23-56(101)102/h31-32,35-42,45-52,57-61,96H,12-30,33-34,76H2,1-11H3,(H,77,81)(H,78,82)(H,79,103)(H,80,110)(H,83,104)(H,84,106)(H,85,105)(H,86,107)(H,87,108)(H,88,109)(H,89,113)(H,90,111)(H,91,112)(H,92,114)(H,99,100)(H,101,102)(H,116,117)/t39-,40-,41-,42+,45-,46-,47-,48-,49-,50-,51-,52-,57-,58-,59-,60-,61-/m0/s1
Chemical Name
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-carboxybutanoyl]amino]pentanedioic acid
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~59.38 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 50 mg/mL (29.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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