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AMG 517

Catalog No. T6379 CAS 659730-32-2

Synonyms: AMG517, AMG-517

AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1.

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AMG 517, CAS 659730-32-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 556.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.85%

Purity: 99.66%

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Description	AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1.
Targets&IC50	TRPV1(capsaicin):0.62 nM, TRPV1(heat activation):1.3 nM, TRPV1(proton):0.76 nM
In vitro	AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced 45Ca2+ influx into human TRPV1-expressing CHO Cells with IC50 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. [1]
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.[1] 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.[2]

Synonyms	AMG517, AMG-517
Molecular Weight	430.4
Formula	C20H13F3N4O2S
CAS No.	659730-32-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL (100 mM)

References and Literature

1. Gavva NR, et al. J Pharmacol Exp Ther, 2007, 323(1), 128-137. 2. Gavva NR, et al. Pain, 2008, 136(1-2), 202-210. 3. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1[J]. Frontiers in Pharmacology. 2021, 11: 2233.

Citations

1. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1. Frontiers in Pharmacology. 2021 Jan 13;11:539261. doi: 10.3389/fphar.2020.539261. eCollection 2020. 2. Zhang M, Jia X, Cheng C, et al.Capsaicin functions as a selective degrader of STAT3 to enhance host resistance to viral infection.Acta Pharmacologica Sinica.2023: 1-12.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Membrane Protein-targeted Compound Library Ion Channel Inhibitor Library ReFRAME Related Library Clinical Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library

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Keywords

AMG 517 659730-32-2 Membrane transporter/Ion channel TRP/TRPV Channel AMG517 Inhibitor inhibit Transient receptor potential channels TRP Channel AMG-517 inhibitor

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