AMG2504
AMG2504 is a TRPA1 antagonist with an IC50 value of 35 nM against human TRPA1. AMG2504 inhibits human TRPA1 activation induced by AITC and noxious cold stimulation. AMG2504 is applicable to research related to chronic pain.
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- CAS. Nr.: 202342-22-1
- Formel: C15H10Cl4N2O3S
- Molecular Weight:440.13
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
hTRPA 35 nM (IC50) |
In Vitro
AMG2504 potently inhibits human TRPA1 with an IC50 of 35 nM. It exhibits no agonist activity against human TRPA1, and shows only extremely low or no antagonist activity against rat TRPA1[2].
AMG2504 potently inhibits AITC (HY-B1515)-induced intracellular calcium influx in CHO cells expressing human TRPA1, with an IC50 of 35 nM, and suppresses AITC-induced inward currents in cells, with an IC50 of 167 nM[3].
AMG2504 inhibits noxious cold stimulus-induced 45Ca2+ uptake in CHO cells expressing human TRPA1, with an IC50 of 105 nM[3].
AMG2504 is selective for human TRPA1, with IC50 values greater than 5 μM against human TRPV1, TRPM8, TRPV3 and TRPV4[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS. Nr. 202342-22-1
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Molecular Weight 440.13
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Formel C15H10Cl4N2O3S
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SMILES
O=C(C1=CC=C([N+]([O-])=O)C=C1)NC(C(Cl)(Cl)Cl)SC2=CC=C(C=C2)Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
[1]. Tanner MR, et al. Differences in ion channel phenotype and function between humans and animal models. Front Biosci (Landmark Ed). 2018;23(1):43-64. Published 2018 Jan 1. [Content Brief]
[2]. Eid SR. Therapeutic targeting of TRP channels--the TR(i)P to pain relief. Curr Top Med Chem. 2011;11(17):2118-30. [Content Brief]
[3]. Klionsky L, et al. Species-specific pharmacology of Trichloro(sulfanyl)ethyl benzamides as transient receptor potential ankyrin 1 (TRPA1) antagonists. Mol Pain. 2007;3:39. Published 2007 Dec 17. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AMG2504 Related Classifications
HY-15058 Related Classifications
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