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Meclinertant

Cat. No. M7330
Meclinertant Structure
Synonym:

SR 48692

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5mg USD 550  USD550 3-4 Weeks
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Quality Control & Documentation
Biological Activity

Meclinertant (SR 48692) is an effective, selective, non-peptide and oral antagonist of active neurotensin receptor (NTS1). Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization in human colon cancer cells, with a pA2 value of 8.13. Meclinertant has anti-anxiety, anti-addiction and memory disorder effects.

Chemical Information
Molecular Weight 587.07
Formula C32H31ClN4O5
CAS Number 146362-70-1
Solubility (25°C) DMSO 11.74 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] Anderson. Life Sci. Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator.

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Keywords: Meclinertant, SR 48692 supplier, Neurotensin Receptor, inhibitors, activators


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