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SBI-553

Cat. No. M10142
SBI-553 Structure
Synonym:

SBI553

Size Price Availability Quantity
5mg USD 330  USD330 In stock
10mg USD 530  USD530 In stock
25mg USD 980  USD980 In stock
50mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

SBI-553 is a potent and effective, brain-penetrant and allosteric modulator of NTR1 with EC50 of 0.34 μM.

Chemical Information
Molecular Weight 450.55
Formula C26H31FN4O2
CAS Number 1849603-72-0
Solubility (25°C) DMSO 55 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] Lauren M Slosky, et al. Trends Pharmacol Sci. Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery

[2] Lauren M Slosky, et al. Cell. β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors

[3] Anthony B Pinkerton, et al. J Med Chem. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators

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