| Identification | Back Directory | [Name]
Valiglurax | [CAS]
1976050-09-5 | [Synonyms]
VU2957
VU-2957
VU 2957
Valiglurax
VU2957, Valiglurax
6-Isoquinolinamine, N-1H-pyrazolo[3,4-b]pyridin-3-yl-1-(trifluoromethyl)- | [Molecular Formula]
C16H10F3N5 | [MDL Number]
MFCD31916243 | [MOL File]
1976050-09-5.mol | [Molecular Weight]
329.28 |
| Chemical Properties | Back Directory | [Boiling point ]
549.9±45.0 °C(Predicted) | [density ]
1.530±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
10.01±0.40(Predicted) | [color ]
Light yellow to yellow | [InChI]
1S/C16H10F3N5/c17-16(18,19)13-11-4-3-10(8-9(11)5-7-20-13)22-15-12-2-1-6-21-14(12)23-24-15/h1-8H,(H2,21,22,23,24) | [InChIKey]
RUEXKBWCUUFJMY-UHFFFAOYSA-N | [SMILES]
FC(F)(F)c1nccc2c1ccc(c2)Nc3n[nH]c4ncccc43 |
| Hazard Information | Back Directory | [Uses]
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease[1]. | [Biological Activity]
Valiglurax is an orally availableCNS penetrantpotent and selective mGlu4 positive allosteric modulator (PAM). | [in vivo]
Valiglurax (VU0652957; 0.3-30 mg/kg; po) reverses haloperidol (HY-14538)-induced catalepsy (HIC) in rats in a dose-dependent manner[1]. | Animal Model: | haloperidol-induced catalepsy (HIC) in rats[1] | | Dosage: | 0.3-30 mg/kg | | Administration: | Oral administration | | Result: | Reversed haloperidol (HY-14538)-induced catalepsy (HIC) in rats in a dose-dependent manner. |
| [References]
[1] Panarese JD, et, al. Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. DOI:10.1021/acsmedchemlett.8b00426 |
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