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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
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

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 386.76
Formula C16H14ClF3N4O2
CAS Number 2304549-73-1
Purity >98%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
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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Keywords: GFB-8438 supplier, TRP Channel, inhibitors

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