HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi and a pIC50 of 9.3 and 9.2, respectively. HTL14242 can be used for the research of parkinson’s disease.

Product information

CAS Number: 1644645-32-8

Molecular Weight: 310.71

Formula: C16H8ClFN4

Chemical Name: 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile

Smiles: N#CC1C=C(Cl)C=C(C=1)C1=CC(=NC=N1)C1=CC=C(F)C=N1

InChiKey: FQAXDSVNYVVQSE-UHFFFAOYSA-N

InChi: InChI=1S/C16H8ClFN4/c17-12-4-10(7-19)3-11(5-12)15-6-16(22-9-21-15)14-2-1-13(18)8-20-14/h1-6,8-9H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 12.5 mg/mL (40.23 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

HTL14242 is stable in rat plasma, inactive at the hERG ion-channel, and has a clean profile in vitro assays of cytotoxicity in HepG2 cells, the TC50 is >90 μM.

In Vivo:

HTL14242 (oral administration; 1, 3, or 10 mg/kg; sacrificed 1 h postdose) emonstrates an excellent, dose-dependent occupancy of mGlu5 receptors from an oral dose, with an estimated ED50 of 0.3 mg/kg. HTL14242 (oral administration; 1 mg/ml) exhibits an oral PK Profile, the t1/2, AUCinf and F% are 6.5 hours, 3946 ng/h/mL and 80%, respectively in dog.

Products are for research use only. Not for human use.