Resiniferatoxin
目录号 : GC12783
Resiniferatoxin是一种选择性 TRPV1 受体激动剂，以不可逆的方式激活TRPV1。
Cas No.:57444-62-9
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
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Cell experiment [1]: |
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Cell lines |
IEC-18 cell line |
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Preparation method |
Cells were treated with different concentrations of RTX for 24 hours as instructed. |
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Reaction Conditions |
0.1-10μM Resiniferatoxin; 24 hours |
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Applications |
Resiniferatoxin at 5–10 μM produced a prolonged cell cycle arrest in G0/G1 phase that was first evident by 6 h and sustained for at least 24 h. |
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Animal experiment [2]: |
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Animal models |
Male Wistar rats |
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Preparation method |
Rats (weighing 240–255 g) underwent L5 spinal nerve ligation, On day 7, rats were injected with 100 µL of Resiniferatoxin 0.002% (2 µg) or vehicle (10% Tween 80, 10% EtOH, 80% normal saline) in the plantar skin of the left hind paw. |
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Dosage form |
100 µL of Resiniferatoxin 0.002% (2 µg); s.c in the plantar skin |
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Applications |
Intraplantar injection of RTX completely alleviates thermal and mechanical hypersensitivity caused by L5 nerve injury. |
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References: [1].Frey MR, Clark JA, et,al.Cell cycle- and protein kinase C-specific effects of resiniferatoxin and resiniferonol 9,13,14-ortho-phenylacetate in intestinal epithelial cells. Biochem Pharmacol. 2004 May 15;67(10):1873-86. doi: 10.1016/j.bcp.2004.02.006. PMID: 15130764. [2]. Javed H, Johnson AM,et,al. Cutaneous Injection of Resiniferatoxin Completely Alleviates and Prevents Nerve-Injury-Induced Neuropathic Pain. Cells. 2022 Dec 14;11(24):4049. doi: 10.3390/cells11244049. PMID: 36552812; PMCID: PMC9776507. |
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Resiniferatoxin (RTX), an ultrapotent capsaicin analog, is a vanilloid agonist that binds to the transient receptor potential channel, vanilloid subfamily member 1 (TRPV1).Resiniferatoxin activates TRPV1 in an irreversible manner. It also can bind and activate members of the PKC family[1-4].
Resiniferatoxin(0.1-10μM; 24 hours) can induce G0/G1 arrest in non-transformed intestinal epithelial cells[4].
Resiniferatoxin (250ng,50µL; s.c) blocks inflammatory heat hyperalgesia when applied directly to the sciatic nerve in a time and dose dependent fashion[5]. Resiniferatoxin treatment increased serum levels of IL-4, IL-10 and IL-13, and it decreases intestinal eosinophilia, however, favours the mastocytosis, promoting T spiralis intestinal expulsion[6]. Cutaneous injection of Resiniferatoxin(100 µL of RTX 0.002% (2 µg); s.c in the plantar skin) completely alleviates and prevents nerve-injury-induced neuropathic pain in rat[7].
References:
[1]. Brown DC. Resiniferatoxin: The Evolution of the "Molecular Scalpel" for Chronic Pain Relief. Pharmaceuticals (Basel). 2016 Aug 11;9(3):47. doi: 10.3390/ph9030047. PMID: 27529257; PMCID: PMC5039500.
[2]. Montell C, Birnbaumer L, et,al. A unified nomenclature for the superfamily of TRP cation channels. Mol Cell. 2002 Feb;9(2):229-31. doi: 10.1016/s1097-2765(02)00448-3. PMID: 11864597.
[3]. Gunthorpe MJ, Benham CD, et,al. The diversity in the vanilloid (TRPV) receptor family of ion channels. Trends Pharmacol Sci 2002, 23:183–191.
[4]. Frey MR, Clark JA, et,al. Cell cycle- and protein kinase C-specific effects of resiniferatoxin and resiniferonol 9,13,14-ortho-phenylacetate in intestinal epithelial cells. Biochem Pharmacol. 2004 May 15;67(10):1873-86. doi: 10.1016/j.bcp.2004.02.006. PMID: 15130764.
[5]. Neubert JK, Mannes AJ, et,al. Perineural resiniferatoxin selectively inhibits inflammatory hyperalgesia. Mol Pain. 2008 Jan 16;4:3. doi: 10.1186/1744-8069-4-3. PMID: 18199335; PMCID: PMC2242785.
[6]. Muñoz-Carrillo JL, Gutiérrez-Coronado O, et,al. Resiniferatoxin promotes adult worm expulsion in Trichinella spiralis-infected rats by Th2 immune response modulation. Parasite Immunol. 2021 Aug;43(8):e12840. doi: 10.1111/pim.12840. Epub 2021 May 10. PMID: 33914935.
[7]. Javed H, Johnson AM, et,al. Cutaneous Injection of Resiniferatoxin Completely Alleviates and Prevents Nerve-Injury-Induced Neuropathic Pain. Cells. 2022 Dec 14;11(24):4049. doi: 10.3390/cells11244049. PMID: 36552812; PMCID: PMC9776507.
Resiniferatoxin (RTX)是一种超强辣椒素类似物，是一种结合瞬时受体电位通道，香草蛋白亚家族成员1 (TRPV1)的香草蛋白激动剂。Resiniferatoxin以不可逆的方式激活TRPV1，它还可以结合和激活PKC家族的成员[1-4]。
Resiniferatoxin(0.1 -10μM;24 h)可诱导未转化肠上皮细胞G0/G1阻滞[4]。
Resiniferatoxin (250ng,50µL;s.c)直接作用于坐骨神经时，可阻断炎症性热痛觉过敏，且具有时间和剂量依赖性[5]。Resiniferatoxin治疗可提高血清IL-4、IL-10和IL-13水平，减少肠道嗜酸性粒细胞，但有利于肥大细胞增生，促进螺旋T虫肠道排出[6]。皮下注射Resiniferatoxin (100µL RTX 0.002% (2 µg); s.c in the plantar skin)完全缓解和预防大鼠神经损伤性神经性疼痛[7]。
| Cas No. | 57444-62-9 | SDF | |
| 化学名 | ((2R,3aR,3bS,6aR,9aR,9bR,10R,11aR)-2-benzyl-6a-hydroxy-8,10-dimethyl-7-oxo-11a-(prop-1-en-2-yl)-3b,6,6a,7,9a,10,11,11a-octahydro-3aH-2,9b-epoxyazuleno[5',4':3,4]benzo[1,2-d][1,3]dioxol-5-yl)methyl 2-(4-hydroxy-3-methoxyphenyl)acetate | ||
| Canonical SMILES | O[C@@]12[C@@H](C=C(C)C2=O)[C@]34O[C@@](O[C@@]5(C(C)=C)C[C@H]4C)(CC6=CC=CC=C6)O[C@@H]5[C@@H]3C=C(COC(CC(C=C7OC)=CC=C7O)=O)C1 | ||
| 分子式 | C37H40O9 | 分子量 | 628.72 |
| 溶解度 | Soluble in DMSO > 10 mM | 储存条件 | Store at -20°C, protect from light |
| 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 | 1.5905 mL | 7.9527 mL | 15.9053 mL |
| 5 mM | 0.3181 mL | 1.5905 mL | 3.1811 mL |
| 10 mM | 0.1591 mL | 0.7953 mL | 1.5905 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。