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SUN11602

Cat. No. M7544
SUN11602  Structure
Size Price Availability Quantity
10mg USD 150  USD150 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

In vitro: SUN11602 prevents glutamate-induced neuronal death in primary cultures of rat cerebrocortical neurons. SUN11602 increases the levels of CALB1 gene expression in cerebrocortical neurons. SUN11602 exerts protective effects on hippocampal neurons through activation of FGFR1 and increases CalB expression. SUN11602 promotes neurite outgrowth of primarily cultured rat hippocampal neurons.

In vivo: In WT mice, SUN11602 increases the levels of newly synthesized Calb in cerebrocortical neurons and suppresses the glutamate-induced rise in intracellular Ca2+. This Ca2+-capturing ability of Calb allows the neurons to survive severe toxic conditions of glutamate. Oral administration of SUN11602 at the midpoint of Aβ1-40 and ibotenate injections attenuate short-term memory impairment in the Y-maze test, as well as spatial learning deficits in the water maze task. In addition, the SUN11602 treatment inhibits the increase of peripheral-type benzodiazepine-binding sites (PTBBS),which are a marker for gliosis.

Protocol (for reference only)
Cell Experiment
Cell lines hippocampal neurons
Preparation method Cerebrocortical neurons are pretreated with vehicle (Hanks’ Balanced Salt Solution), SUN11602, bFGF, or the other growth factors for 24 h prior to the onset of glutamate toxicity. Subsequently, 10 μL of the MTT solution (5 mg/mL) is added to each well (200 μL of culture medium) of the microplates. Neurons in each well are then dried for 24 h, and 200 μL of DMSO is poured into all of the wells in order to dissolve the reaction products thoroughly for the MTT assay
Concentrations 10 μM
Incubation time 24 h
Animal Experiment
Animal models F344/DuCrj rats
Formulation
Dosages 0.1, 1, and 10 mg/kg
Administration orally
Chemical Information
Molecular Weight 451.6
Formula C26H37N5O2
CAS Number 704869-38-5
Solubility (25°C) 37 mg/mL in DMSO
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] Borroto-Escuela DO, et al. Front Cell Neurosci. Disturbances in the FGFR1-5-HT1A Heteroreceptor Complexes in the Raphe-Hippocampal 5-HT System Develop in a Genetic Rat Model of Depression.

[2] Ogino R, et al. Brain Res. SUN11602 has basic fibroblast growth factor-like activity and attenuates neuronal damage and cognitive deficits in a rat model of Alzheimer's disease induced by amyloid β and excitatory amino acids.

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