1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)

TFLLR-NH2(TFA) 

Cat. No.: HY-P0226A Purity: 99.29%
Handling Instructions

TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

TFLLR-NH2(TFA) Chemical Structure

TFLLR-NH2(TFA) Chemical Structure

CAS No. : 1313730-19-6

Size Price Stock Quantity
1 mg USD 216 In-stock
Estimated Time of Arrival: December 31
5 mg USD 864 In-stock
Estimated Time of Arrival: December 31
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Other Forms of TFLLR-NH2(TFA):

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.

IC50 & Target

EC50: 1.9 μM (PAR1)[1]

In Vitro

PAR1 agonists stimulate concentration-dependent increases in [Ca2+]i and in the proportions of neurones. The maximal increase in [Ca2+]i above basal is detected in response to 10 μm TF-NH2 (peak 196.5±20.4 nM, n=25) when 50–80% of identified neurones responded[1]. SW620 cells cultured in the supernatant of TFLLR-NH2-activated platelets upregulate E-cadherin expression and downregulate the vimentin expression. In the in vitro platelet culture system, a TFLLR-NH2 dose-dependent increase of secreted TGF-β1 is detected in the supernatant[2].

In Vivo

Injection of TF-NH2 into the rat paw stimulates a marked and sustained oedema. An NK1R antagonist and ablation of sensory nerves with capsaicin inhibit oedema by 44% at 1 h and completely by 5 h. In wild-type but not PAR1−/− mice, TF-NH2 stimulates Evans blue extravasation in the bladder, oesophagus, stomach, intestine and pancreas by 2–8 fold. Extravasation in the bladder, oesophagus and stomach is abolished by an NK1R antagonist[1]. TFp-NH2 produces notable contraction at 3-50 μM and relaxation at 0.3-50 μM, in the absence of apamin. The concentration-response curve for TFp-NH2-induced contraction is remarkably shifted left, when the TFp-NH2-induced relaxation is blocked by apamin at 0.1 μM[3].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Mice are anaesthetized with isofluorane, and saline or TF-NH2 (3 μmol/kg in 25 μL physiological saline) is injected into the lateral tail vein. Evans blue (33.3 mg/kg in 50 μL saline) is co-injected with the peptide. Mice are perfused transcardially at 10 min after administration of TF-NH2 with physiological saline containing 20 u/mL heparin at a pressure of 80-100 mmHg for 2-3 min. Excised tissues are incubated in 1 mL of formamide for 48 h, and Evans blue content is measured spectrophotometrically at 650 nm[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

761.83

Formula

C₃₃H₅₄F₃N₉O₈

CAS No.

1313730-19-6

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TFLLR-NH2(TFA)
Cat. No.:
HY-P0226A
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TFLLR-NH2(TFA)

Cat. No.: HY-P0226A