HC-030031 is a TRPA1 selective antagonist. TRPA1 may play an important role in acute formalin and CFA induced pain. HC-030031 does not block currents mediated by TRPV1, TRPV3, TRPV4 hERG, or NaV1.2 channels. The selective TRPA1 antagonist HC-030031 can be used in cells or delivered to animals orally, by inhalation, or by injection. Oral administration of HC-030031 reduced AITC-induced nocifensive behaviors at a dose of 100 mg/kg in the rat. Moreover, oral HC-030031 (100 mg/kg) significantly reversed mechanical hypersensitivity in the more chronic models of Complete Freunds Adjuvant (CFA)-induced inflammatory pain and the spinal nerve ligation model of neuropathic pain.
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Source | Cancer Res (2013). Figure 1. HC-030031 |
| Method | i.g. | |
| Cell Lines | C57BL/6 mice | |
| Concentrations | 300 mg/kg | |
| Incubation Time | 60 minutes | |
| Results | Systemic treatment with HC-030031 (300 mg/kg, i.g.) at day 7 after treatment with bortezomib (0.2 or 0.5 mg/kg, i.p.) completely but transiently reverted both mechanical hyperalgesia and cold allodynia |
| Molecular Weight | 355.39 |
| Formula | C18H21N5O3 |
| CAS Number | 349085-38-7 |
| Solubility (25°C) | DMSO 27 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] McNamara CR, et al. Proc Natl Acad Sci U S A. TRPA1 mediates formalin-induced pain.
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