VU0652957
Modify Date: 2024-09-16 16:58:06
VU0652957 structure
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Common Name | VU0652957 | ||
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| CAS Number | 1976050-09-5 | Molecular Weight | 329.286 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C16H10F3N5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of VU0652957VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours). |
| Name | VU0652957 |
|---|
| Description | VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours). |
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| References | References 1. Panarese JD, et al. Bioorg Med Chem Lett. 2018 Nov 1. pii: S0960-894X(18)30853-9. View Related Products by Target mGluR |
| Molecular Formula | C16H10F3N5 |
|---|---|
| Molecular Weight | 329.286 |