WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522645
CAS#: 1883711-97-4
Description: AM-0902 is a potent and selective Transient Receptor Potential A1 (TRPA1) Antagonist Demonstrating Potent in Vivo Activity with pharmacokinetic properties allowing for >30-fold coverage of the rat TRPA1 IC50 in vivo. AM-0902 showed rTRPA1 45Ca2+ Flux IC50=0.071 microM and hTRPA1 45Ca2+ Flux IC50=0.131 microM. AM-0902 demonstrated dose-dependent inhibition of AITC-induced flinching in rats, validating its utility as a tool for interrogating the role of TRPA1 in in vivo pain models.
Hodoodo Cat#: H522645
Name: AM-0902
CAS#: 1883711-97-4
Chemical Formula: C17H15ClN6O2
Exact Mass: 370.09
Molecular Weight: 370.797
Elemental Analysis: C, 55.07; H, 4.08; Cl, 9.56; N, 22.67; O, 8.63
Synonym: AM-0902; AM 0902; AM0902.
IUPAC/Chemical Name: 1-((3-(4-chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1,7-dihydro-6H-purin-6-one
InChi Key: AWJBWNUUODWOKQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H15ClN6O2/c1-23-9-19-16-15(23)17(25)24(10-20-16)8-14-21-13(22-26-14)7-4-11-2-5-12(18)6-3-11/h2-3,5-6,9-10H,4,7-8H2,1H3
SMILES Code: O=C1N(CC2=NC(CCC3=CC=C(Cl)C=C3)=NO2)C=NC4=C1N(C)C=N4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | AM-0902 is a transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. |
| In vitro activity: | TBD |
| In vivo activity: | This study tested the effect of intrathecal administration of 1 μg and 5 μg of AM-0902, and these doses were assessed on the basis of the effective concentration observed from spinal cord slice recordings and the estimated cerebrospinal fluid volume (300 μl) in adult rats. Intrathecal injection of AM-0902 attenuated tactile allodynia, mechanical hyperalgesia, and heat hyperalgesia in the CFA-treated rats in a dose-dependent manner (Fig. 8B). In contrast, intrathecal injection of 1 μg and 5 μg of AM-0902 had no significant effect on the paw withdrawal thresholds in vehicle-treated rats (Fig. 8C). Reference: J Neurochem. 2019 May; 149(3): 381–398. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6483867/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 93.5 | 252.27 |
The following data is based on the product molecular weight 370.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Huang Y, Chen SR, Chen H, Pan HL. Endogenous transient receptor potential ankyrin 1 and vanilloid 1 activity potentiates glutamatergic input to spinal lamina I neurons in inflammatory pain. J Neurochem. 2019 May;149(3):381-398. doi: 10.1111/jnc.14677. Epub 2019 Mar 26. PMID: 30716174; PMCID: PMC6483867. 2. Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4. PMID: 26942860. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Huang Y, Chen SR, Chen H, Pan HL. Endogenous transient receptor potential ankyrin 1 and vanilloid 1 activity potentiates glutamatergic input to spinal lamina I neurons in inflammatory pain. J Neurochem. 2019 May;149(3):381-398. doi: 10.1111/jnc.14677. Epub 2019 Mar 26. PMID: 30716174; PMCID: PMC6483867. 2. Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4. PMID: 26942860. |
1: Huang Y, Chen SR, Chen H, Pan HL. Endogenous transient receptor potential ankyrin 1 and vanilloid 1 activity potentiates glutamatergic input to spinal lamina I neurons in inflammatory pain. J Neurochem. 2019 May;149(3):381-398. doi: 10.1111/jnc.14677. Epub 2019 Mar 26. PMID: 30716174; PMCID: PMC6483867.
2: Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4. PMID: 26942860.
