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HC-067047

Cat. No. M8239
HC-067047 Structure
Size Price Availability Quantity
10mg USD 122  USD122 In stock
25mg USD 265  USD265 In stock
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Quality Control
Biological Activity

HC-067047 is a potent, selective inhibitor of hTRPV4. The compound inhibits human, rat and mouse TRPV4 with IC50 values of 48, 133 and 17 nM, respectively. HC-067047 does not inhibit other TRPV isoforms at concentrations up to 5 μM. HC-067047 inhibits hERG channel and the menthol receptor TRPM8 with IC50 values of 370 and 780 nM, respectively.

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 471.51
Formula C26H28F3N3O2
CAS Number 883031-03-6
Purity 99.64%
Solubility DMSO: ≥15 mg/mL
Storage at -20°C
References

[1] Shotaro Michinaga, et al. Pharmacological Inhibition of Transient Receptor Potential Vanilloid 4 Reduces Vasogenic Edema after Traumatic Brain Injury in Mice

[2] Fumio Nakagawa, et al. Modification of TRPV4 activity by acetaminophen

[3] Maki Yoneda, et al. PIEZO1 and TRPV4, which Are Distinct Mechano-Sensors in the Osteoblastic MC3T3-E1 Cells, Modify Cell-Proliferation

[4] Fabiana C Dias, et al. The selective TRPV4 channel antagonist HC-067047 attenuates mechanical allodynia in diabetic mice

[5] Zhouqing Wang, et al. TRPV4-induced inflammatory response is involved in neuronal death in pilocarpine model of temporal lobe epilepsy in mice

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Keywords: HC-067047 supplier, TRP Channel, inhibitors

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