| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
PAR1 agonists cause concentration-dependent increases in [Ca2+]i and neuronal ratios. In response to 10 μ m TF-NH2, 50–80% of the identified neurons showed the greatest increase in [Ca2+]i above basal values (peak 196.5±20.4 nM, n=25) [1]. Expression of E-cadherin was upregulated and vimentin was downregulated in SW620 cells cultured in TFLLR-NH2 activated platelet supernatants. A dose-dependent rise in TGF-β1 secreted by TFLLR-NH2 was found in the supernatant of an in vitro platelet culture system [2].
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| ln Vivo |
Rat paws were injected with TF-NH2, which caused a notable and long-lasting edema. Capsaicin and NK1R antagonist-induced sensory nerve ablation reduced edema by 44% in 1 hour and by 100% in 5 hours. TF-NH2 increased Evans blue extravasation 2- to 8-fold in the bladder, esophagus, stomach, intestine, and pancreas in wild-type mice, but not in PAR1−/− animals. Extravasation in the stomach, esophagus, and bladder can be completely eliminated by NK1R antagonists [1]. TFp-NH2 induced considerable contraction at 3-50 μM and significant relaxation at 0.3-50 μM in the absence of apamin. The concentration-response curve of TFp-NH2-induced contraction markedly moved to the left when 0.1 μM apamin inhibited TFp-NH2-induced relaxation [3].
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| References |
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| Molecular Formula |
C33H54F3N9O8
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|---|---|
| Molecular Weight |
761.83257818222
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| Exact Mass |
761.404
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| CAS # |
1313730-19-6
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| Related CAS # |
TFLLR-NH2;197794-83-5
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| PubChem CID |
71311619
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
53
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C(F)(F)(F)C(=O)O.[C@@H](NC(=O)[C@@H](N)[C@H](O)C)(C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N)CCCNC(N)=N)CC1C=CC=CC=1
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| InChi Key |
QVNWOGSDGQDGHP-MKVNCOEFSA-N
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| InChi Code |
InChI=1S/C31H53N9O6.C2HF3O2/c1-17(2)14-22(27(43)37-21(26(33)42)12-9-13-36-31(34)35)38-28(44)23(15-18(3)4)39-29(45)24(16-20-10-7-6-8-11-20)40-30(46)25(32)19(5)41;3-2(4,5)1(6)7/h6-8,10-11,17-19,21-25,41H,9,12-16,32H2,1-5H3,(H2,33,42)(H,37,43)(H,38,44)(H,39,45)(H,40,46)(H4,34,35,36);(H,6,7)/t19-,21+,22+,23+,24+,25+;/m1./s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~131.26 mM)
DMSO : ~100 mg/mL (~131.26 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (43.75 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3126 mL | 6.5631 mL | 13.1263 mL | |
| 5 mM | 0.2625 mL | 1.3126 mL | 2.6253 mL | |
| 10 mM | 0.1313 mL | 0.6563 mL | 1.3126 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.
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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