UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with EC50 of 4.2 nM. UCSF924 has high affinity for DRD4 with Ki of 3 nM, but no measurable affinity for D2, D3, or the F261V/L328F D4 mutant. For Gαi/o signaling, UCSF924 was 7.4-fold biased against arrestin.

Physicochemical Properties

Molecular Formula	C20H22N2O2
Molecular Weight	322.400885105133
Exact Mass	322.168
CAS #	1434515-70-4
PubChem CID	72901200
Appearance	White to off-white solid powder
LogP	3.3
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Heavy Atom Count	24
Complexity	443
Defined Atom Stereocenter Count	0
InChi Key	RPHDOVLXDYWDGF-UHFFFAOYSA-N
InChi Code	InChI=1S/C20H22N2O2/c1-15-8-9-19-18(12-15)20(23)13-16(22-19)14-21-10-5-11-24-17-6-3-2-4-7-17/h2-4,6-9,12-13,21H,5,10-11,14H2,1H3,(H,22,23)
Chemical Name	6-methyl-2-[(3-phenoxypropylamino)methyl]-1H-quinolin-4-one
Synonyms	UCSF924; UCSF-924
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]. D4 dopamine receptor high-resolution structures enable the discovery of selective agonists. Science. 2017 Oct 20;358(6361):381-386.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~155.09 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.1017 mL	15.5087 mL	31.0174 mL
	5 mM	0.6203 mL	3.1017 mL	6.2035 mL
	10 mM	0.3102 mL	1.5509 mL	3.1017 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.