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.
For research use only. We do not sell to patients.
- CAS No.: 202342-22-1
- Formula: C15H10Cl4N2O3S
- Molecular Weight:440.13
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hTRPA 35 nM (IC50) |
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.
Chemical Information
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CAS No. 202342-22-1
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Molecular Weight 440.13
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AMG2504 Related Classifications
HY-15058 Related Classifications
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