659730-32-2
Amg 517
CAS: 659730-32-2
Molecular Formula: C20H13F3N4O2S
659730-32-2 - Names and Identifiers
659730-32-2 - Physico-chemical Properties
| Molecular Formula | C20H13F3N4O2S |
| Molar Mass | 430.4 |
| Density | 1.458 |
| Melting Point | 227℃ |
| pKa | 10.19±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | AMG 517 inhibits CAP-(500 nM), acid (pH 5.0), or heat (45°C) induced |
| In vivo study | AMG 517 oral treatment, resulting in increased plasma concentrations, this effect exists in a dose-dependent manner, also reduce the number of clot withdrawal induced by Capsaicin treatment, this effect also exists in a dose-dependent manner. The lowest effective dose (MED) for AMG 517 was found to be 0.3 mg/kg based on the statistically significant difference in the number of withdrawal between the control group and the Capsaicin group. The corresponding plasma concentration of AMG 517 is 90 to 100 ng/mL. Treatment with AMG 517(3 mg/kg) for 24 hours significantly reduced Capsaicin-induced withdrawal. AMG 517 acts on CFA pain model to inhibit thermal hyperalgesia. AMG 517 acts in rodents, dogs and monkeys, but not in TRPV1 knockout mice, causing hyperthermia. Interestingly, TRPV1 selective antagonist-induced hyperthermia was attenuated by repeated administration of these antagonists to rats, dogs, and monkeys, as well as TRPV1 knockout mice, without a decrease in body temperature. |
659730-32-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.323 ml | 11.617 ml | 23.234 ml |
| 5 mM | 0.465 ml | 2.323 ml | 4.647 ml |
| 10 mM | 0.232 ml | 1.162 ml | 2.323 ml |
| 5 mM | 0.046 ml | 0.232 ml | 0.465 ml |
Last Update：2024-01-02 23:10:35
659730-32-2 - Reference Information
| biological activity | AMG-517 is a potent, selective antagonist of TRPV1, proton and thermal activation, IC50 0.76 nM, 0.62 nM and 1.3 nM, respectively. |
| Target | TargetValue TRPV1 () 1 nM-2 nM |
| Target | Value |
| TRPV1 () | 1 nM-2 nM |
| in vitro study | AMG 517 inhibits CAP-(500 nM), acid (pH 5.0), or heat (45°C) induced |
| in vivo study | AMG 517 oral treatment resulted in an increase in plasma concentration, which was dose-dependent, the number of clot retraction induced by Capsaicin treatment was also reduced, and this effect was also dose-dependent. The lowest effective dose (MED) for AMG 517 was found to be 0.3 mg/kg based on the statistically significant difference in the number of withdrawal between the control group and the Capsaicin group. The corresponding plasma concentration of AMG 517 is 90 to 100 ng/mL. Treatment with AMG 517(3 mg/kg) for 24 hours significantly reduced Capsaicin-induced withdrawal. AMG 517 acts on CFA pain model to inhibit thermal hyperalgesia. AMG 517 acts in rodents, dogs and monkeys, but not in TRPV1 knockout mice, causing hyperthermia. Interestingly, TRPV1 selective antagonist-induced hyperthermia was attenuated by repeated administration of these antagonists to rats, dogs, and monkeys, as well as TRPV1 knockout mice, without a decrease in body temperature. |
Last Update：2024-04-09 21:54:55
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Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
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Multiple SpecificationsSpot supply
Product Name: AMG 517 Visit Supplier Webpage Request for quotationCAS: 659730-32-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: Amg 517 Visit Supplier Webpage Request for quotationCAS: 659730-32-2
Tel: 18301782025
Email: 3008007409@qq.com
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