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

Cat. No.	Product name	Field of application
DC73469	ML353	ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.
DC49647	MNI137	MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization.
DC44955	RO0711401	RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.
DC28990	Decoglurant	Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant.
DC28980	Biphenylindanone A	Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders.
DC28200	LY367385	LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
DC11437	VU0652957	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).
DC7843	JNJ 42153605	JNJ 42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
DC7016	JNJ40411813	For the detailed information of JNJ40411813, the solubility of JNJ40411813 in water, the solubility of JNJ40411813 in DMSO, the solubility of JNJ40411813 in PBS buffer, the animal experiment (test) of JNJ40411813, the cell expriment (test) of JNJ40411813, the in vivo, in vitro and clinical trial test of JNJ40411813, the EC50, IC50,and Affinity of JNJ40411813, Please contact DC Chemicals..