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Chemical Structure : VU0652957
Catalog No.: PC-35879Not For Human Use, Lab Use Only.
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.
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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).
| M.Wt | 329.286 | |
| Formula | C16H10F3N5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Panarese JD, et al. Bioorg Med Chem Lett. 2018 Nov 1. pii: S0960-894X(18)30853-9.
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