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HC-030031

Cat. No. M2087
HC-030031 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 30  USD30 In stock
10mg USD 45  USD45 In stock
50mg USD 117  USD117 In stock
100mg USD 175  USD175 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 355.39
Formula C18H21N5O3
CAS Number 349085-38-7
Purity 99.66%
Solubility DMSO 27 mg/mL
Storage at -20°C
References

[1] Lennertz RC, et al. PLoS One. TRPA1 mediates mechanical sensitization in nociceptors during inflammation.

[2] Eid SR, et al. Mol Pain. HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity.

[3] McNamara CR, et al. Proc Natl Acad Sci U S A. TRPA1 mediates formalin-induced pain.

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Keywords: HC-030031 supplier, TRP Channel, inhibitors

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