[CAS NO. 1644645-32-8] HTL14242

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PRODUCTS SPECIFICATIONS [1644645-32-8]

Catalog

HY-W062697

Brand

MCE

CAS

1644645-32-8

DESCRIPTION [1644645-32-8]

Overview

MDL	-
Molecular Weight	310.71
Molecular Formula	C16H8ClFN4
SMILES	N#CC1=CC(C2=NC=NC(C3=NC=C(F)C=C3)=C2)=CC(Cl)=C1

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

Summary

HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pK _i and a pIC ₅₀ of 9.3 and 9.2, respectively ^[1] . HTL14242 can be used for the research of parkinson’s disease ^[2] .

IC50 & Target

mGlu ₅

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 TC ₅₀ 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 mGlu ₅ receptors from an oral dose, with an estimated ED ₅₀ of 0.3 mg/kg ^[1] .
HTL14242 (oral administration; 1 mg/ml) exhibits an oral PK Profile, the t _1/2 , AUC _inf 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03785054	Heptares Therapeutics Limited\|Covance	Healthy	November 14, 2018	Phase 1
NCT04462263	Heptares Therapeutics Limited	Healthy	June 29, 2020	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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

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 >> 90% corn oil

Solubility: ≥ 1.25 mg/mL (4.02 mM); Clear solution

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