SSD114 hydrochloride

SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.

Product information

CAS Number: 2319790-02-6

Molecular Weight: 387.83

Formula: C18H21ClF3N3O

Chemical Name: N-cyclohexyl-4-methoxy-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine; chlorohydrogen

Smiles: Cl.COC1=CC(=NC(NC2CCCCC2)=N1)C1C=CC(=CC=1)C(F)(F)F

InChiKey: YXQSTPASDICGCA-UHFFFAOYSA-N

InChi: InChI=1S/C18H20F3N3O.ClH/c1-25-16-11-15(12-7-9-13(10-8-12)18(19,20)21)23-17(24-16)22-14-5-3-2-4-6-14;/h7-11,14H,2-6H2,1H3,(H,22,23,24);1H

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 130 mg/mL (335.20 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:

In the presence of 10 µM GABA, SSD114 hydrochloride at 25 µM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride, added at 15 and 30 µM, induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 µM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 µM, reaching 161±5.09% over the basal value .

In Vivo:

The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice.

References:

1. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.

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