KNT-127 is a potent and specific delta opioid receptor agonist (activator) that is administered systemically. KNT-127 is selective for delta receptors (Ki for opioid mu, delta, and kappa receptors are 21.3, 0.16, and 153 nM, respectively). KNT-127 increases dopamine and L-glutamate release in the striatum, nucleus accumbens, and median prefrontal cortex. Has antidepressant-like effects.

Physicochemical Properties

Molecular Formula	C24H24N2O2
Molecular Weight	372.459566116333
Exact Mass	372.1838
CAS #	1256921-89-7
PubChem CID	52942137
Appearance	Off-white to light yellow solid powder
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	0
Heavy Atom Count	28
Complexity	628
Defined Atom Stereocenter Count	3
SMILES	O[C@@]12CC3=CC4C=CC=CC=4N=C3C[C@@]31C1C=C(C=CC=1C[C@H]2N(C)CC3)O
Synonyms	KNT-127 KNT127 KNT 127
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]. Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration. Bioorg Med Chem Lett. 2010;20(21):6302-6305. [2]. Novel δ1-receptor agonist KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. Neuropharmacology. 2012;62(5-6):2057-2067.

Solubility Data

Solubility (In Vitro)

DMSO : ~25 mg/mL (~67.12 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (3.36 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 12.5 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6849 mL	13.4243 mL	26.8485 mL
	5 mM	0.5370 mL	2.6849 mL	5.3697 mL
	10 mM	0.2685 mL	1.3424 mL	2.6849 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.