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CFMTI 

Cat. No. M30738
CFMTI  Structure
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Biological Activity

CFMTI inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a, with IC50s of 2.6 and 2.3 nM, respectively.

Chemical Information
Molecular Weight 349.36
Formula C19H16FN5O
CAS Number 864864-17-5
Form Solid
Solubility (25°C) DMSO 3.7 mg/mL (ultrasonic and warming and heat to 60°C)
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] A Lesner, et al. Biochem Biophys Res Commun. Design, chemical synthesis and kinetic studies of trypsin chromogenic substrates based on the proteinase binding loop of Cucurbita maxima trypsin inhibitor (CMTI-III)

[2] K Bolewska, et al. FEBS Lett. Synthesis, cloning and expression in Escherichia coli of a gene coding for the Met8-->Leu CMTI I--a representative of the squash inhibitors of serine proteinases

[3] J Rózycki, et al. Biol Chem Hoppe Seyler. Analogues of Cucurbita maxima trypsin inhibitor III (CMTI-III) with elastase inhibitory activity

[4] R Krishnamoorthi, et al. Biochemistry. Structural consequences of the natural substitution, E9K, on reactive-site-hydrolyzed squash (Cucurbita maxima) trypsin inhibitor (CMTI), as studied by two-dimensional NMR

[5] K Rolka, et al. Biol Chem Hoppe Seyler. New analogues of Cucurbita maxima trypsin inhibitor III (CMTI III) with simplified structure

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Keywords: CFMTI  supplier, GluR, inhibitors, activators

 
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