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AMG-0347

Catalog No. T29968 CAS 946615-43-6

Synonyms: UNII-CD7L9290QR

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

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AMG-0347, CAS 946615-43-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 397.00
5 mg	In stock	$ 970.00
10 mg	In stock	$ 1,290.00
25 mg	In stock	$ 1,950.00
50 mg	In stock	$ 2,620.00
100 mg	In stock	$ 3,530.00
1 mL * 10 mM (in DMSO)	In stock	$ 995.00

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Purity: 99.7%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.
In vitro	'The inhibitory effects of AMG0347 on the activation of TRPV1 channels by heat (45°C), protons (pH5), or capsaicin (500 nM) were evaluated using the 45 Ca2+ uptake assay in Chinese hamster ovary cells stably expressing rat or human TRPV1 channels.[1] AMG0347 demonstrated potent and selective antagonism against TRPV1 in vitro. Concentration-dependent inhibition was observed with IC50 values of 0.2 nM for heat-induced activation, 0.8 nM for proton-induced activation, and 0.7 nM for capsaicin-induced activation of rat TRPV1 channels. AMG0347 did not exhibit blocking activity against other TRP channels, including TRPV2, TRPV3, TRPV4, TRP ankyrin-1, and TRP melastatin-8, with IC50 values of 10 μM.[1]'
In vivo	AMG0347 did not change the withdrawal threshold to mechanical stimulation or the guarding pain score. The withdrawal latency to heat increased from 3 h through 1 day after AMG0347 administration. AMG0347 prevented the decreases in heat withdrawal latency and mechanical withdrawal threshold caused by capsaicin infiltration and prevented the increase in activity caused by intrathecal capsaicin injection.[2]

Synonyms	UNII-CD7L9290QR
Molecular Weight	445.48
Formula	C24H26F3N3O2
CAS No.	946615-43-6

Storage

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

Solubility Information

DMSO: 27.5 mg/mL (61.73 mM)

References and Literature

1. Steiner AA, et al. Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors. J Neurosci. 2007;27(28):7459-7468. 2. Wu C, et al. Effect of AMG0347, a transient receptor potential type V1 receptor antagonist, and morphine on pain behavior after plantar incision. Anesthesiology. 2008;108(6):1100-1108. 3. Montell C, et al. Thermoregulation: channels that are cool to the core. Curr Biol. 2007;17(20):R885-R887. 4. Steiner AA, et al. Nonthermal activation of transient receptor potential vanilloid-1 channels in abdominal viscera tonically inhibits autonomic cold-defense effectors. J Neurosci. 2007;27(28):7459-7468.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets

D-GsMTx4 TFA HC067047 Hydrochloride(883031-03-6 free base) 2-Aminoethyl diphenylborinate ASP7663 AMG2850 ML204 SN 2 PF-4840154

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Keywords

AMG-0347 946615-43-6 Membrane transporter/Ion channel TRP/TRPV Channel AMG 0347 UNII-CD7L9290QR AMG0347 inhibitor inhibit

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