| Identification | Back Directory | [Name]
JT010 | [CAS]
917562-33-5 | [Synonyms]
JT010
2-Chloro-N-[4-(4-methoxyphenyl)-2-thiazolyl]-N-(3-methoxypropyl)acetamide
Acetamide, 2-chloro-N-[4-(4-methoxyphenyl)-2-thiazolyl]-N-(3-methoxypropyl)- | [Molecular Formula]
C16H19ClN2O3S | [MDL Number]
MFCD08899142 | [MOL File]
917562-33-5.mol | [Molecular Weight]
354.85 |
| Chemical Properties | Back Directory | [Boiling point ]
487.4±55.0 °C(Predicted) | [density ]
1.265±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
powder | [pka]
2.59±0.10(Predicted) | [color ]
white to beige | [InChI]
1S/C16H19ClN2O3S/c1-21-9-3-8-19(15(20)10-17)16-18-14(11-23-16)12-4-6-13(22-2)7-5-12/h4-7,11H,3,8-10H2,1-2H3 | [InChIKey]
KZMAWJRXKGLWGS-UHFFFAOYSA-N | [SMILES]
O=C(N(C1=NC(C2=CC=C(OC)C=C2)=CS1)CCCOC)CCl |
| Hazard Information | Back Directory | [Description]
JT010 is a transient receptor potential ankyrin 1 (TRPA1) agonist (EC50 = 0.65 nM in a calcium influx assay). It is selective for TRPA1 over TRP vanilloid 1 (TRPV1), TRPV3, TRPV4, TRP canonical channel 5 (TRPC5), TRP melastatin 2 (TRPM2), and TRPM8 channels at 1 μM. | [Uses]
JT010 is a potent and selective TRPA1 channel activator (EC50 = 65 nM); activates the TRPA1 channel by covalently and site-selectively binding to Cys621. Exhibits selectivity for TRPA1 over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50 values are >1 μM). | [Biochem/physiol Actions]
JT010 is a non-cytotoxic and highly stable (>90% remains after 2 h in 1 mM DTT or 2-mercaptoethanol) chloroacetamido warhead-carrying thiazole derivative that acts as a potent and TRPA1-selective channel activator via covalent modification of TRPA1 active site Cys621. JT0101 stimulates calcium influx in TRPA1-transfected HEK293 cells in a dose-dependent manner (EC50?= 650 pM) with excellent selectivity over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50?>1 μM). | [in vivo]
JT010 (0.4 mg/kg, i.v., 60 or 5 min prior to left coronary artery occlusion and 5 min prior to onset of the reperfusion) and A-967079 (HY-108463) have small opposing effects on myocardial infarct size in male rats[6].
| [storage]
Store at +4°C | [References]
[1] JUNICHIRO TAKAYA. A Potent and Site-Selective Agonist of TRPA1[J]. Journal of the American Chemical Society, 2015, 137 50: 15859-15864. DOI: 10.1021/jacs.5b10162 |
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