Shanghai Nianxing Industrial Co., Ltd
China
Product Name: TFLLR-NH2
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Huang

DC Chemicals Limited
China
Product Name: TFLLRN-NH2
Price: ￥Inquiry/100mg ￥Inquiry/250mg ￥Inquiry/1g
Purity: 98.0%
Stocking Period: 10 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: TFLLR-NH2
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Taiwan Oyi peptide Co. Ltd
China
Product Name: H-THR-PHE-LEU-LEU-ARG-NH2
Price: $Inquiry/1mg $Inquiry/100kg
Purity: 98.0%
Stocking Period: 1 Day
Contact: Vinnie

197794-83-5

197794-83-5 structure

197794-83-5 structure

Name: (Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt
Chemical Name: tfllr-nh2
CAS Number: 197794-83-5
Molecular Formula: C₃₁H₅₃N₉O₆
Molecular Weight: 647.80900
Catalog: Peptides
Create Date: 2018-07-18 21:56:08
Modify Date: 2024-01-03 05:46:16
TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.

Name	tfllr-nh2
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

Description	TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Protease-Activated Receptor (PAR) Research Areas >> Cardiovascular Disease Peptides
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.

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