| Identification | Back Directory | [Name]
2-(1,3-DIMETHYL-2,6-DIOXO-1,2,3,6-TETRAHYDRO-7H-PURIN-7-YL)-N-(4-ISOPROPYLPHENYL)ACETAMIDE | [CAS]
349085-38-7 | [Synonyms]
CS-828
HC 030031
HC 030031 1G
TOSLAB 829227
HC030031; HC 030031
TrpA1 Antagonist, HC-030031
HC-030031;HC 030031;HC030031
TrpA1 Antagonist, HC-030031 - CAS 349085-38-7 - Calbiochem
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(4-propan-2-ylphenyl)acetamide
2-(1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)-N-(4-isopropylphenyl)acetamide
2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6
-tetrahydro-purin-7-yl)-N-isoprop
yl-phenyl)-acetamide
2-(1,3-DIMETHYL-2,6-DIOXO-1,2,3,6-TETRAHYDRO-7H-PURIN-7-YL)-N-(4-ISOPROPYLPHENYL)ACETAMIDE
1,2,3,6-Tetrahydro-1,3-diMethyl-N-[4-(1-Methylethyl)phenyl]-2,6-dioxo-7H-purine-7-acetaMide
7H-Purine-7-acetamide, 1,2,3,6-tetrahydro-1,3-dimethyl-N-[4-(1-methylethyl)phenyl]-2,6-dioxo- | [Molecular Formula]
C18H21N5O3 | [MDL Number]
MFCD02007349 | [MOL File]
349085-38-7.mol | [Molecular Weight]
355.39 |
| Chemical Properties | Back Directory | [Melting point ]
221-223°C | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
White solid | [pka]
13.71±0.70(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | [InChIKey]
HEQDZPHDVAOBLN-UHFFFAOYSA-N |
| Hazard Information | Back Directory | [Description]
Transient receptor potential cation channel A1 (TRPA1) is an ankyrin-like ion channel which acts as a sensor for chemical irritants, pain, and cold. It is activated by allyl isothiocyanate (AITC), formalin, hydrogen peroxide, tear gas, and other compounds.1,2,3 HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50s = 6.2 and 5.3 μM, respectively).2 It does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels.2 HC-030031 can be used in cells or delivered to animals orally, by inhalation, or by injection.4,2,5,6 Oral administration (100 mg/kg) of HC-030031 significantly reversed mechanical hypersensitivity in rat models of chronic inflammatory or neuropathic pain, while local injection (100 μg) into inflamed mouse hind paws attenuated mechanical, but not heat, hypersensitivity.4,6 | [Chemical Properties]
White Solid | [Uses]
A TRPA1 (transient receptor potential) selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. | [Biological Activity]
Selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx (IC 50 values are 6.2 and 5.3 μ M respectively). Does not block currents mediated by TRPV1, TRPV3, TRPV4, hERG or Na V 1.2 channels. Inhibits AITC- and formalin-induced flinching in vivo . | [Biochem/physiol Actions]
HC-030031 is a selective TRPA1 channel blocker, antagonizing formalin-evoked calcium influx and formalin-induced pain. IC50 is 5 μM. TRPA1 antagonism is a promising therapeutic target for chronic inflammatory or neurogenic pain. | [storage]
Room temperature | [References]
1) McNamara et al. (2007), TRPA1 mediates formalin-induced pain; Proc. Natl. Acad. Sci., 104 13525 |
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