AMG-517 |
| رقم الكتالوجGC13003 |
AMG-517 هو أحد مضادات مستقبلات الفانيليا القوية والاختيارية -1 (TRPV1) مع IC 50 من 0.5 نانومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 659730-32-2
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment[1]: | |
|
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. |
|
Reacting condition |
1-2 nM |
|
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]: | |
|
Clinical samples |
Healthy adults |
|
Dosage form |
Oral administration, 2, 5 and 10 mg |
|
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. |
|
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. | |
| Cas No. | 659730-32-2 | SDF | |
| Chemical Name | 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 | ||
| Formula | C20H13F3N4O2S | M.Wt | 430.4 |
| الذوبان | ≥ 21.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3234 mL | 11.6171 mL | 23.2342 mL |
| 5 mM | 464.7 μL | 2.3234 mL | 4.6468 mL |
| 10 mM | 232.3 μL | 1.1617 mL | 2.3234 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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