AMG-517
(Synonyms: N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺) 目录号 : GC13003
A TRPV1 antagonist
Cas No.:659730-32-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment[1]: | |
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Cell lines |
CHO cells |
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Preparation method |
The solubility of this compound in DMSO is > 21.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1-2 nM |
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Applications |
AMG 517 is a selective antagonist of both rat and human TRPV1 with dissociation constant values of 4.2 and 6.2 nM, respectively. AMG 517 effectively and completely inhibited capsaicin, proton, and heat activation of TRPV1 in vitro. AMG 517 potently inhibited capsaicin-, acid-, and heat-induced Ca2+ uptake into CHO cells expressing TRPV1 with IC50 values of 1 to 2 nM. |
| Clinical experiment [2]: | |
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Clinical samples |
Healthy adults |
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Dosage form |
Oral administration, 2, 5 and 10 mg |
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Application |
AMG 517 blocked TRPV1 and elicited a generally plasma concentration-dependent hyperthermia in healthy humans. AMG 517 caused hyperthermia by increasing thermogenesis and inducing tail skin vasoconstriction, indicating that TRPV1 regulates metabolic heat production and vasomotor tone in humans. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Gavva N R, Bannon A W, Hovland D N, et al. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 323(1): 128-137. [2]. Gavva N R, Treanor J J S, Garami A, et al. Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans[J]. Pain, 2008, 136(1): 202-210. | |
AMG-517 is an antagonist of TRPV1 channel with IC50 value of 1-2 nM [1].
TRP1, transient receptor potential cation channel subfamily V member 1, is a subfamily of the transient receptor potential protein group and plays an important role in detecting and regulating body temperature or sensing pain. TRPV1 can be activated by diverse stimuli, including several ingredients of the inflammatory soup which leads to a painful, burning sensation. It is reported that TRPV1 channel may play a pivotal role in many diseases like SIRS [1] [2].
AMG-517 is a TRPV1 antagonist. When tested with stable CHO cell lines expressing TRPV1, treated with AMG-517 inhibited the activation of TRPV1 [1].
In C57BL/6 mice with SIRS induced by LPS, pretreatment with AMG-517 (210 µg/kg) markedly decreased the survival rate and increased the risk of mortality [2]. When tested with Trpv1-/- mice, intraperitoneally treated with AMG-517 (256 nmol/kg) inhibited TRPV1 with inducing hyperthermia in a dose-dependent manner [3]. In capsaicin-induced flinch male Sprague-Dawley rats, oral administration of AMG-517 markedly decreased the number of flinches in a dose-dependent manner [1].
References:
[1].Gavva, N.R., et al., Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther, 2007. 323(1): p. 128-37.
[2].Wanner, S.P., et al., Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory. Cell Cycle, 2012. 11(2): p. 343-9.
[3].Garami, A., et al., Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J Neurosci, 2010. 30(4): p. 1435-40.
| Cas No. | 659730-32-2 | SDF | |
| 别名 | N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺 | ||
| 化学名 | N-[4-[6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]oxy-1,3-benzothiazol-2-yl]acetamide | ||
| Canonical SMILES | CC(=O)NC1=NC2=C(C=CC=C2S1)OC3=NC=NC(=C3)C4=CC=C(C=C4)C(F)(F)F | ||
| 分子式 | C20H13F3N4O2S | 分子量 | 430.4 |
| 溶解度 | ≥ 21.5mg/mL in DMSO | 储存条件 | Store 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 | 2.3234 mL | 11.6171 mL | 23.2342 mL |
| 5 mM | 0.4647 mL | 2.3234 mL | 4.6468 mL |
| 10 mM | 0.2323 mL | 1.1617 mL | 2.3234 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。