TFLLR-NH2
目录号 : GC17444
A peptide agonist of PAR1
Cas No.:197794-83-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | 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 (33.3mg/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. | |
TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
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].
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].
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.
| Cas No. | 197794-83-5 | SDF | |
| 化学名 | (S,Z)-2-((Z)-((S)-2-((Z)-((2S,3R)-2-amino-1,3-dihydroxybutylidene)amino)-1-hydroxy-3-phenylpropylidene)amino)-N-((S,Z)-1-(((S)-5-guanidino-1-hydroxy-1-iminopentan-2-yl)imino)-1-hydroxy-4-methylpentan-2-yl)-4-methylpentanimidic acid | ||
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])[C@@](O)([H])C)([H])CC1=CC=CC=C1)([H])CC(C)C)([H])/C(O)=N/[C@@](C(O)=N)([H])CCCNC(N)=N)C | ||
| 分子式 | C31H53N9O6 | 分子量 | 647.82 |
| 溶解度 | Soluble to 1 mg/ml in 20% acetonitrile / sterile water | 储存条件 | Desiccate at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5436 mL | 7.7182 mL | 15.4364 mL |
| 5 mM | 0.3087 mL | 1.5436 mL | 3.0873 mL |
| 10 mM | 0.1544 mL | 0.7718 mL | 1.5436 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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