N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517
Amg 517
CAS: 659730-32-2
Molecular Formula: C20H13F3N4O2S
N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517 - Names and Identifiers
N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517 - 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. |
N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517 - 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
N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517 - 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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Product Name: Amg 517 Visit Supplier Webpage Request for quotationCAS: 659730-32-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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