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GFB-8438

Cat. No. M10927
GFB-8438 Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
25mg USD 360  USD360 In stock
50mg USD 570  USD570 In stock
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Quality Control & Documentation
Biological Activity

GFB-8438 is a potent subtype selective TRPC5 inhibitor against hTRPC5 and hTRPC4 IC50 0.18 and 0.29 μM, respectively. GFB-8438 has good selectivity for TRPC6, other members of the TRP family, NaV1.5, and limited activity against hERG channels. Protective effect of GFB-8438 on mouse podocytes.

Chemical Information
Molecular Weight 386.76
Formula C16H14ClF3N4O2
CAS Number 2304549-73-1
Solubility (25°C) DMSO ≥ 60 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] Zhuang Zhang, et al. Bioorg Med Chem Lett. Discovery of pyrroledione analogs as potent transient receptor potential canonical channel 5 inhibitors

[2] Alireza Baradaran-Heravi, et al. J Biol Chem. Nonselective TRPC channel inhibition and suppression of aminoglycoside-induced premature termination codon readthrough by the small molecule AC1903

[3] Maolin Yu, et al. ACS Med Chem Lett. Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model

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