| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
AMG 517 (AMG-517; AMG517) is a novel, potent and selective TRPV1 (vanilloid receptor-1) antagonist with potential anti-inflammatory activity. It antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. The TRPV1 channel plays a suppressive role in the systemic inflammatory response syndrome (SIRS) by inhibiting production of tumor necrosis factor (TNF)α and possibly by other mechanisms. TRPV1 antagonists may decrease the resistance of older patients to infection and sepsis. When tested with stable CHO cell lines expressing TRPV1, treated with AMG-517 inhibited the activation of TRPV1.
| ln Vitro |
AMG 517 maintained efficacy in the capsaicin- and acid-mediated tests with IC50 values of 0.9 and 0.5 nM[1]. AMG 517 reduces capsaicin, pH 5, and heat-induced45Ca2+ uptake into cells expressing TRPV1 with IC50 values of 1 to 2 nM. AMG 517 inhibits capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells equally. AMG 517 suppresses native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 ± 0.2 nM. AMG 517 is a competitive antagonist of both rat and human TRPV1 with dissociation constant (Kb) values of 4.2 and 6.2 nM, respectively[2].
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| ln Vivo |
In a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED= 0.83 mg/kg, po) and a rodent "on-target" biochemical challenge model (capsaicin-induced flinch, ED50=0.33 mg/kg po), AMG 517 has been demonstrated to be effective[1]. The minimally effective dose of AMG 517 is 0.3 mg/kg, and the corresponding plasma concentration is 90 ng/mL. At 21 hours following CFA injection, oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner. AMG 517 induces brief hyperthermia in dogs, monkeys, and rodents. AMG 517 causes a high dose-dependent induction of hyperthermia; increases in body temperature of 0.5, 0.6, and 1.6°C are correlated with doses of 0.3, 1, and 3 mg/kg, respectively. Within 10 to 20 hours, the body temperatures of rats given all dosages of AMG 517 recover to baseline[2].
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| References |
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| Molecular Formula |
C20H13F3N4O2S
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| Molecular Weight |
430.4
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| Exact Mass |
430.071
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| CAS # |
659730-32-2
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| Related CAS # |
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| PubChem CID |
16007367
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
227ºC
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| Index of Refraction |
1.645
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| LogP |
5.41
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
603
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YUTIXVXZQIQWGY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13F3N4O2S/c1-11(28)26-19-27-18-15(3-2-4-16(18)30-19)29-17-9-14(24-10-25-17)12-5-7-13(8-6-12)20(21,22)23/h2-10H,1H3,(H,26,27,28)
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| Chemical Name |
N-[4-[6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl]oxy-1,3-benzothiazol-2-yl]acetamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% Tween 80 : 30 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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