VU2957|Valiglurax|CAS 1976050-09-5|DC Chemicals

Cas No.:	1976050-09-5
Chemical Name:	N-(1H-pyrazolo[3,4-b]pyridin-3-yl)-1-(trifluoromethyl)isoquinolin-6-amine
Synonyms:	VU2957;Valiglurax
SMILES:	FC(F)(F)C1=NC=CC2=C1C=CC(NC3=NNC4=C3C=CC=N4)=C2
Formula:	C₁₆H₁₀F₃N₅
M.Wt:	329.286
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1. Panarese JD, et al. Bioorg Med Chem Lett. 2018 Nov 1. pii: S0960-894X(18)30853-9.

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:

1. Panarese JD, et al. Bioorg Med Chem Lett. 2018 Nov 1. pii: S0960-894X(18)30853-9.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

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