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

HTL14242 (Synonyms: HTL0014242)

Cat. No.: HY-W062697
Handling Instructions

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.

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

HTL14242 Chemical Structure

HTL14242 Chemical Structure

CAS No. : 1644645-32-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi and a pIC50 of 9.3 and 9.2, respectively[1]. HTL14242 can be used for the research 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
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 Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2184 mL 16.0922 mL 32.1844 mL
5 mM 0.6437 mL 3.2184 mL 6.4369 mL
10 mM 0.3218 mL 1.6092 mL 3.2184 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (8.05 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (8.05 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
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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