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VU 0361737

Cat. No. M2576
VU 0361737 Structure
Synonym:

ML-128

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 80  USD80 In stock
25mg USD 170  USD170 In stock
50mg USD 285  USD285 In stock
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Quality Control & Documentation
Biological Activity

VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively. VU 0361737 displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.

Chemical Information
Molecular Weight 262.69
Formula C13H11ClN2O2
CAS Number 1161205-04-4
Solubility (25°C) DMSO 40 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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Keywords: VU 0361737, ML-128 supplier, GluR, inhibitors, activators


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