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SB 366791

Cat. No. M7264
SB 366791 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 85  USD85 In stock
25mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

SB 366791 is a potent, selective and competitive vanilloid TRPV1 receptor antagonist (pA2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB1 and CB2 receptors, voltage-gated Ca2+ channels and the hyperpolarization-activated current (Ih).

Chemical Information
Molecular Weight 287.75
Formula C16H14ClNO2
CAS Number 472981-92-3
Solubility (25°C) DMSO 28.77 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] Alessi, et al. J Biol Chem. PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo.

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