VU0652957 (VU2957, Valiglurax)

Chemical Structure : VU0652957

CAS No.: 1976050-09-5

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货号: 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.

规格	价格	库存
10 mg	￥1280	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg		Get quote

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生物&药学活性

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.
VU0652957 (VU2957, Valiglurax) 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.
VU0652957 (VU2957, Valiglurax) also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours).

物理化学性质&存储条件

分子量	329.286
分子式	C16H10F3N5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(1H-pyrazolo[3,4-b]pyridin-3-yl)-1-(trifluoromethyl)isoquinolin-6-amine

参考文献

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