PAR 4 (1-6) (TFA)(Synonyms: GYPGQV TFA)

PAR 4 (1-6) (TFA);(Synonyms: GYPGQV TFA)

PAR 4 (1-6) TFA (GYPGQV TFA) 是一种六胜肽,它是蛋白酶激活受体 4 (PAR4) 的一个片段,并且能作为 PAR4 特异性的抑制剂。

PAR 4 (1-6) (TFA)amp;;(Synonyms: GYPGQV TFA)

PAR 4 (1-6) (TFA) Chemical Structure

规格 是否有货
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生物活性

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

Protease-Activated Receptor-1, PAR-1 Agonist;

Protease-Activated Receptor-1, PAR-1 Agonist 是一种选择性蛋白酶激活受体1 (PAR-1) 激动肽。Protease-Activated Receptor-1, PAR-1 Agonist 对应于PAR1配体,可通过该受体选择性地模拟凝血酶的作用。

Protease-Activated Receptor-1, PAR-1 Agonistamp;;

Protease-Activated Receptor-1, PAR-1 Agonist Chemical Structure

CAS No. : 141136-85-8

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Protease-Activated Receptor-1, PAR-1 Agonist 的其他形式现货产品:

Protease-Activated Receptor-1, PAR-1 Agonist TFA

生物活性

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

Protease-Activated Receptor-3 (PAR-3) (1-6), human;

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), humanamp;;

Protease-Activated Receptor-3 (PAR-3) (1-6), human Chemical Structure

CAS No. : 1872435-09-0

规格 是否有货
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250 mg ; 询价 ;
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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(Synonyms: PAR-1 agonist peptide Thrombin Receptor Activator Peptide 6)

TRAP-6;(Synonyms: PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6) 纯度: 99.74%

TRAP-6 (PAR-1 agonist peptide),一种多肽片段,是选择性的蛋白酶激活受体 1 (PAR1) 激动剂。TRAP-6 通过凝血酶受体激活人血小板。TRAP-6 对 PAR4 无活性。

TRAP-6amp;;(Synonyms: PAR-1 agonist peptide;  Thrombin Receptor Activator Peptide 6)

TRAP-6 Chemical Structure

CAS No. : 141136-83-6

规格 价格 是否有货 数量
10;mM;*;1 mL in Water ¥1760 In-stock
10 mg ¥1600 In-stock
25 mg ¥3520 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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TRAP-6 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Peptidomimetic Library
  • Targeted Diversity Library
  • Peptide Library

生物活性

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.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 100 mg/mL (133.53 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3353 mL 6.6767 mL 13.3535 mL
5 mM 0.2671 mL 1.3353 mL 2.6707 mL
10 mM 0.1335 mL 0.6677 mL 1.3353 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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

Protease-Activated Receptor-1, PAR-1 Agonist TFA; 纯度: 99.08%

Protease-Activated Receptor-1, PAR-1 Agonist TFA 是一种选择性蛋白酶激活受体1 (PAR-1) 激动肽。Protease-Activated Receptor-1, PAR-1 Agonist TFA 对应于 PAR1 配体,可通过该受体选择性地模拟凝血酶的作用。

Protease-Activated Receptor-1, PAR-1 Agonist TFAamp;;

Protease-Activated Receptor-1, PAR-1 Agonist TFA Chemical Structure

规格 价格 是否有货 数量
10 mg ¥4250 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Protease-Activated Receptor-1, PAR-1 Agonist TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Peptide Library

生物活性

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.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

H2O : 6.67 mg/mL (7.61 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1404 mL 5.7018 mL 11.4035 mL
5 mM 0.2281 mL 1.1404 mL 2.2807 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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 TFA

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA; 纯度: 98.85%

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA 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 TFAamp;;

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide[1].

IC50 Target

PAR-3[1]

分子量

760.76

Formula

C31H47F3N10O9

Sequence Shortening

TFRGAP-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

参考文献
  • [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

TFLLR-NH2;

TFLLR-NH2是选择性的PAR1激动剂,EC50值为1.9 μM。

TFLLR-NH2amp;;

TFLLR-NH2 Chemical Structure

CAS No. : 197794-83-5

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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TFLLR-NH2 的其他形式现货产品:

TFLLR-NH2(TFA)

生物活性

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.