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VU 0357121

Cat. No. M3126
VU 0357121 Structure
Size Price Availability Quantity
10mg USD 90  USD90 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

VU0357121 does not have PAM activity at other mGluR subtypes, neither binds at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.

Chemical Information
Molecular Weight 305.32
Formula C17H17F2NO2
CAS Number 433967-28-3
Solubility (25°C) DMSO 50 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] Christine E Wells, et al. Déjà vu experiences in anxiety

[2] Marija Bošnjak Pašić, et al. Many Faces of Déjà Vu: a Narrative Review

[3] Maarten P Bebelman, et al. Biogenesis and function of extracellular vesicles in cancer

[4] Rosa E Boeschoten, et al. Prevalence of depression and anxiety in Multiple Sclerosis: A systematic review and meta-analysis

[5] P-P A Vergroesen, et al. Mechanics and biology in intervertebral disc degeneration: a vicious circle

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