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Pico145

Cat. No. M14284
Pico145 Structure
Synonym:

HC-608

Size Price Availability
5mg USD 350  USD350 4-7 Days
10mg USD 550  USD550 4-7 Days
25mg USD 1100  USD1100 4-7 Days
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Quality Control & Documentation
Biological Activity

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

Chemical Information
Molecular Weight 524.88
CAS Number 1628287-16-0
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Ningyong Xu, et al. Impact of Na+ permeation on collective migration of pulmonary arterial endothelial cells

[2] David J Wright, et al. Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site

[3] Aisling Minard, et al. Potent, selective, and subunit-dependent activation of TRPC5 channels by a xanthine derivative

[4] Katsuhiko Muraki, et al. Na + entry through heteromeric TRPC4/C1 channels mediates (-)Englerin A-induced cytotoxicity in synovial sarcoma cells

[5] Hussein N Rubaiy, et al. Pico145 - powerful new tool for TRPC1/4/5 channels

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Keywords: Pico145, HC-608 supplier, TRP Channel, inhibitors, activators


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