1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. HTL14242

HTL14242 (Synonyms: HTL0014242)

Cat. No.: HY-W062697
Handling Instructions

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

For research use only. We do not sell to patients.

HTL14242 Chemical Structure

HTL14242 Chemical Structure

CAS No. : 1644645-32-8

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Description

HTL14242 (HTL0014242) is an advanced, orally active and potent mGlu5 NAM with a pKi and pIC50 value of 9.3 and 9.2, respectively[1]. HTL14242 can be used for the study of Parkinson’s disease[2].

IC50 & Target[1]

mGlu5

 

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[1].

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[1].
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[1].

Animal Model: Dog (PK study)[1]
Dosage: 3, 10 and 30 mg/kg
Administration: Oral administration; single dose
Result: Had a good PK characteristics in dogs.
Molecular Weight

310.71

Formula

C₁₆H₈ClFN₄

CAS No.

1644645-32-8

SMILES

N#CC1=CC(C2=NC=NC(C3=NC=C(F)C=C3)=C2)=CC(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vivo:
  • 1.

    HTL14242 is dissolve in 10% DMA + 10% Solutol HS15 + 80% saline.

References
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Keywords:

HTL14242HTL0014242HTL 14242HTL-14242HTL 0014242HTL-0014242mGluRMetabotropic glutamate receptorsParkinson’s diseaseGERDHuntingdon’s diseasefragile X syndromemGlu5NAMInhibitorinhibitorinhibit

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HTL14242
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