[CAS NO. 659730-32-2] AMG-517
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PRODUCTS SPECIFICATIONS [659730-32-2]
Store
Catalog
SLK-S7115
Brand
Selleck
CAS
659730-32-2
DESCRIPTION [659730-32-2]
Overview
| MDL | MFCD14584859 |
|---|---|
| Molecular Weight | 430.4 |
| Molecular Formula | C20H13F3N4O2S |
| SMILES | CC(NC1=NC2=C(OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C=CC=C2S1)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
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 |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4647 mL |
Description
AMG 517 is a potent and selective antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with of 0.76 nM, 0.62 nM and 1.3 nM， respectively.
Features
Does not activate TRPV1 at concentrations ≤40 μM (measured by 45Ca uptake into TRPV1-expressing cells), indicating that it is not a partial agonist.
Targets
| TRPV1 [1] |
| 1 nM-2 nM |
In vitro
AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced Ca influx into human TRPV1-expressing CHO Cells with of 0.76 nM, 0.62 nM and 1.3 nM. AMG 517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG 517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 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. AMG 517 is a highly selective TRPV1 antagonist. The IC50 value for AMG 517 is >20 μM against 2-APB-activated TRPV2 and TRPV3, 4-αPDD-activated TRPV4, allyl isothiocyanate-activated TRPA1, and icilin-activated TRPM8 in cell-based assays that measure agonist-induced increases in intracellular calcium in CHO cells recombinantly expressing the appropriate TRP channel.
In vivo
Oral administration of AMG 517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. The minimally effective dose (MED), based on a statistically significant difference in number of flinches from the vehicle versus capsaicin-administered group, is 0.3 mg/kg for AMG 517. The corresponding plasma concentrations are 90 to 100 ng/mL for AMG 517. AMG 517 (3 mg/kg) exhibits significant reductions in capsaicin-induced flinch up to 24 h after dosing. AMG 517 blocks thermal hyperalgesia in CFA model of pain. AMG 517 elicits hyperthermia in rodents, dogs and monkeys but not in TRPV1 knockout mice. Interestingly, hyperthermia evoked by TRPV1-selective antagonists is attenuated after repeated dosing of these antagonists to rats, dogs and monkeys, and TRPV1 knockout mice does not exhibit an impairment of thermoregulation.
References
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