VU 6005649
Tocris Bioscience, part of Bio-Techne | Catalog # 6893
Positive allosteric modulator of mGlu7 and mGlu8 receptors; also NK1 antagonist; brain penetrant
Key Product Details
Description
Positive allosteric modulator of mGlu7 and mGlu8 receptors; also NK1 antagonist; brain penetrant
Product Description
VU 6005649 is a positive allosteric modulator of mGlu7 and mGlu8 receptors (EC50 = 0.65 μM and 2.6 μM for mGlu7 and mGlu8, respectively). Displays >3.8 fold selectivity for mGlu7 and mGlu8 over other mGlu receptors (EC50 >10 μM for mGlu1,2,3,4,5,6). Also NK1 receptor antagonist (Ki= 650 nM, IC50 = 3.4 μM). Brain penetrant.Product Specifications
Molecular Weight
357.28
Formula
C16H12F5N3O
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
CAS Number
2137047-43-7
PubChem ID
131954513
InChI Key
NYBZCKAQIIPSDS-UHFFFAOYSA-N
SMILES
COC1=C(F)C(F)=C(C=C1)C1=C2N=C(C)C=C(N2N=C1C)C(F)(F)F
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.73 | 100 | |
| Ethanol | 17.86 | 50 |
Preparing Stock Solutions
for VU 6005649
The following data is based on the product molecular weight 357.28
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.80 mL | 13.99 mL | 27.99 mL |
| 5 mM | 0.56 mL | 2.80 mL | 5.60 mL |
| 10 mM | 0.28 mL | 1.40 mL | 2.80 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Abe Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines. ACS.Med.Chem.Lett. 2017 PMID: 29057060
Product Specific Notices for VU 6005649
For research use only
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