1976050-09-5
1976050-09-5 structure
- Name: VU0652957
- Chemical Name: VU0652957
- CAS Number: 1976050-09-5
- Molecular Formula: C16H10F3N5
- Molecular Weight: 329.286
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2020-01-12 08:10:50
- Modify Date: 2024-09-16 16:58:06
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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).
| 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). |
|---|---|
| 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 |