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Vanilloid receptor antagonist 1 

Cat. No. M30774
Vanilloid receptor antagonist 1  Structure
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Biological Activity

Vanilloid receptor antagonist 1 is a potent vanilloid receptor TRPV1 antagonist.

Chemical Information
Molecular Weight 305.33
Formula C18H15N3O2
CAS Number 871814-52-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
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] Amanda Spring de Almeida, et al. Eur J Pharmacol. TRP channels in cancer pain

[2] Mircea Iftinca, et al. Drugs. TRPV1-Targeted Drugs in Development for Human Pain Conditions

[3] Zhouqing Wang, et al. Cell Death Dis. TRPV4-induced inflammatory response is involved in neuronal death in pilocarpine model of temporal lobe epilepsy in mice

[4] Mojgan Aghazadeh Tabrizi, et al. Med Res Rev. Medicinal Chemistry, Pharmacology, and Clinical Implications of TRPV1 Receptor Antagonists

[5] Yoonji Lee, et al. Expert Opin Ther Pat. Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014)

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Keywords: Vanilloid receptor antagonist 1  supplier, TRP Channel, inhibitors, activators

 
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