2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. TFLLR-NH2

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

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TFLLR-NH2 Chemical Structure

TFLLR-NH2 Chemical Structure

CAS No. : 197794-83-5

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TFLLR-NH2 Related Antibodies

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Description

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

IC50 & Target

PAR1

1.9 μM (EC50)

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].

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

TFLLR-NH2 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

647.81

Formula

C31H53N9O6
CAS No.
Sequence

Thr-Phe-Leu-Leu-Arg-NH2
Sequence Shortening

TFLLR-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Animal Administration
[1]

Mice: 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
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TFLLR-NH2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TFLLR-NH2197794-83-5Protease Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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