(Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt

Modify Date: 2024-01-03 05:46:16

(Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt Structure
(Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt structure
Common Name (Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt
CAS Number 197794-83-5 Molecular Weight 647.80900
Density N/A Boiling Point N/A
Molecular Formula C31H53N9O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt


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

 Names

Name tfllr-nh2
Synonym More Synonyms

  Biological Activity

Description TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
Related Catalog
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].
Animal Admin 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].
References

[1]. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br J Pharmacol. 2001 Aug;133(7):975-87.

[2]. Kawabata A, et al. Characterization of the protease-activated receptor-1-mediated contraction and relaxation in the rat duodenal smooth muscle.

[3]. Jia Y, et al. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620. Oncol Rep. 2015 Jun;33(6):2681-8.

 Chemical & Physical Properties

Molecular Formula C31H53N9O6
Molecular Weight 647.80900
Exact Mass 647.41200
PSA 267.64000
LogP 2.87230
Storage condition -20℃

 Synonyms

H-THR-PHE-LEU-LEU-ARG-NH2
TFLLR-AMIDE
THR-PHE-LEU-LEU-ARG-NH2
REF DUPL: H-Thr-Phe-Leu-Leu-Arg-NH2
Top Suppliers:I want be here




Get all suppliers and price by the below link:

(Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt suppliers


Price: $216/1mg

Reference only. check more (Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt price