Lu AF32615
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1050 | Check With Us |
500mg | $1600 | Check With Us |
1g | $2400 | Check With Us |
Cat #: V24476 CAS #: 125404-04-8 Purity ≥ 99%
Description: Lu AF32615 is a brain-penetrant positive allosteric modulators (PAMs) of the mGlu4 receptor.
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Molecular Weight (MW) | 197.24 |
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Molecular Formula | C12H11N3 |
CAS No. | 125404-04-8 |
Protocol | In Vitro | In the rat mGlu4 PAM in vitro assay the EC50 of TCN238 (Compound 11) is 1 μM which is comparable to the human assay. TCN238 is screened in rat and human mGlu5 assays, the IC50 of 11 is >30 μM on human mGlu5and >10 μM on rat mGlu5. TCN238 is run in a receptor screening panel of 68 targets and no activity is observed at ≥50% at 10 μM for any of the receptors. In CaCo-2 cells, TCN238 is found to have good permeability with no apparent efflux issue |
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In Vivo | TCN238 is highly CNS penetrant with a concentration of 33.8 μM in the brain. The plasma protein binding in rats is measured as 90% bound. The metabolic stability of TCN238 is assessed in rat and human microsomes and found to be 62% and 83% hepatic blood flow. The limited stability translated into a high in vivo clearance in rats of 75 mL/min/kg and TCN238 has a moderate volume of distribution (2.7 L/kg) with a short mean residence time (0.6 h) when dosed at 2 mg/kg via intravenous injection. TCN238 is orally bioavailable and 30 min following administration of a30 mg/kg dose, the plasma concentration is found to be 11.6 μM |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 5.0700 mL | 25.3498 mL | 50.6997 mL | 101.3993 mL |
5mM | 1.0140 mL | 5.0700 mL | 10.1399 mL | 20.2799 mL |
10mM | 0.5070 mL | 2.5350 mL | 5.0700 mL | 10.1399 mL |
20mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 5.0700 mL |
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