[1]. inase-activated receptors differentially modulate in vitro invasion of human pancreatic adenocarcinoma PANC-1 cells in correlation with changes in the expression of CDC42 protein. Pancreas. 2014 Jan; 43(1): 10.1097/MPA.0b013e31829f0b81.
TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
IC50 Target
EC50: 1.9 μM (PAR1)[1]
体外研究 (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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
647.81
Formula
C31H53N9O6
CAS 号
197794-83-5
Sequence
Thr-Phe-Leu-Leu-Arg-NH2
Sequence Shortening
TFLLR-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[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.
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.
参考文献
[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.
PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR4). PAR 4 (1-6) TFA acts as a PAR4-specific agonist[1].
IC50 Target
PAR4[1]
Formula
C28H41N7O9.xC2HF3O2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. H Andersen, et al. Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci U S A. 1999 Sep 28;96(20):11189-93.
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].
IC50 Target
PAR-1[1]
体外研究 (In Vitro)
Protease-Activated Receptor-1, PAR-1 Agonist induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells expressing PAR1 endogeneously. On the cellular level, Protease-Activated Receptor-1, PAR-1 Agonist and thrombin prompted HT-29 cell migration and matrix adhesion by a PKCepsilon-dependent mechanism as concluded because of the inhibition of PAR1-mediated effects by the PKC inhibitor bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT but not by the PKC inhibitor Gö 6976[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
762.90
Formula
C35H58N10O9
CAS 号
141136-85-8
Sequence
Thr-Phe-Leu-Leu-Arg-Asn
Sequence Shortening
TFLLRN
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Stefanie Gödecke, et al. Thrombin-induced ATP release from human umbilical vein endothelial cells. Am J Physiol Cell Physiol. 2012 Mar 15;302(6):C915-23.
[2]. Heider I, et al. PAR1-type thrombin receptor stimulates migration and matrix adhesion of human colon carcinoma cells by a PKCepsilon-dependent mechanism. Oncol Res. 2004;14(10):475-482.
Protease-Activated Receptor-3 (PAR-3) (1-6), human 是一个蛋白酶活化受体 3 (PAR-3) 的激动剂肽。
Protease-Activated Receptor-3 (PAR-3) (1-6), human Chemical Structure
CAS No. : 1872435-09-0
规格
是否有货
100 mg
;
询价
;
250 mg
;
询价
;
500 mg
;
询价
;
* Please select Quantity before adding items.
Protease-Activated Receptor-3 (PAR-3) (1-6), human 的其他形式现货产品:
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA
生物活性
Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide[1].
IC50 Target
PAR-3[1]
分子量
646.74
Formula
C29H46N10O7
CAS 号
1872435-09-0
Sequence Shortening
TFRGAP-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Liora Segal, et al. Proteinase-activated receptors differentially modulate in vitro invasion of human pancreatic adenocarcinoma PANC-1 cells in correlation with changes in the expression of CDC42 protein. Pancreas. 2014 Jan; 43(1): 10.1097/MPA.0b013e31829f0b81.
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4[1].
IC50 Target
PAR1[1]
体外研究 (In Vitro)
TRAP-6 (0.01-10 μM) triggers calcium mobilization in Xenopus oocytes heterologously expressing PAR1[1]. TRAP-6 (0.01-10 μM; 30 min) activates human platelets[1]. TRAP-6 (100 μM) does not cause the platelets of rabbits or rats to change shape, aggregate, release granule contents, or form thromboxane[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
TRAP (1 mg/kg; i.v.) produces a biphasic response in blood pressure in inactin-anesthetized rats[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
748.87
Formula
C34H56N10O9
CAS 号
141136-83-6
Sequence
Ser-Phe-Leu-Leu-Arg-Asn
Sequence Shortening
SFLLRN
中文名称
凝血酶受体激活肽6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Kahn ML, et, al. Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. J Clin Invest. 1999 Mar;103(6):879-87.
[2]. Kinlough-Rathbone RL, et, al. Rabbit and rat platelets do not respond to thrombin receptor peptides that activate human platelets. Blood. 1993 Jul 1;82(1):103-6.
[3]. Chintala MS, et, al. Disparate effects of thrombin receptor activating peptide on platelets and peripheral vasculature in rats. Eur J Pharmacol. 1998 May 22;349(2-3):237-43.
Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].
体外研究 (In Vitro)
Protease-Activated Receptor-1, PAR-1 Agonist induces activation of protein kinase C isoenzymes alpha and epsilon in human HT-29 colon carcinoma cells expressing PAR1 endogeneously. On the cellular level, Protease-Activated Receptor-1, PAR-1 Agonist and thrombin prompted HT-29 cell migration and matrix adhesion by a PKCepsilon-dependent mechanism as concluded because of the inhibition of PAR1-mediated effects by the PKC inhibitor bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT but not by the PKC inhibitor Gö 6976[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
876.92
Formula
C37H59F3N10O11
Sequence
Thr-Phe-Leu-Leu-Arg-Asn
Sequence Shortening
TFLLRN
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Stefanie Gödecke, et al. Thrombin-induced ATP release from human umbilical vein endothelial cells. Am J Physiol Cell Physiol. 2012 Mar 15;302(6):C915-23.
[2]. Heider I, et al. PAR1-type thrombin receptor stimulates migration and matrix adhesion of human colon carcinoma cells by a PKCepsilon-dependent mechanism. Oncol Res. 2004;14(10):475-482.
