(R)-ML375 ((R)-VU0483253) is the enantiomer of ML375. (R)-ML375 is essentially inactive against M5 mAChR (hM5, IC50>30 μM).

Physicochemical Properties

Molecular Formula	C23H15CLF2N2O2
Molecular Weight	424.83
CAS #	1488362-56-6
Appearance	Solid powder
Synonyms	(R)-VU0483253
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). J Med Chem. 2013 Nov 27;56(22):9351-5.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (235.39 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (5.88 mM) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (these cosolvents are added from left to right, one by one), clear solution; ultrasonic dissolution can obtain a 2.5 mg/mL clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then continue to add 450 μL saline to make up to 1 mL. *Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in 100 mL of ddH₂O to obtain a clear solution. Solubility in formula 2: 2.5 mg/mL (5.88 mM) in 10% DMSO 90% Corn Oil (these co-solvents are added one by one from left to right), clear solution; Ultrasonic dissolution can obtain a 2.5 mg/mL clear solution. This solution can be used as appropriate for animal experiments with an experimental period of more than half a month. . For example, if you need to prepare 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3539 mL	11.7694 mL	23.5388 mL
	5 mM	0.4708 mL	2.3539 mL	4.7078 mL
	10 mM	0.2354 mL	1.1769 mL	2.3539 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.