Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
LY2795050 is a novel, potent and selective κ-opioid Receptor (KOR) antagonist with an IC50 of 0.72 nM. It has the potential to be used as a PET tracer to image KOR in vivo.
Targets |
KOR ( Ki = 0.72 nM ); KOR ( Kb = 0.63 nM )
|
---|---|
ln Vitro |
LY2795050 exhibits antagonist activity with a Kb value of 0.63 nM and high affinity for the KOR with a Ki value of 0.72 nM[1].
|
ln Vivo |
LY2795050 (i.p., 0.032-0.1 mg/kg, 30 min) prevents dose-dependent grooming deficits caused by U50,488 in male and female mice[2]. Some behavioral effects of LY2795050 (i.p., 0.032-0.1 mg/kg, 0-150 min) exhibit sexual dimorphism[2].
|
Animal Protocol |
C57BL/6J mice (gonadally intact, adult, male and female)
0.032-0.1 mg/kg i.p., 0.032-0.1mg/kg, 30 min |
References |
|
Molecular Formula |
C23H22CLN3O2
|
---|---|
Molecular Weight |
407.893
|
Exact Mass |
407.14
|
Elemental Analysis |
C, 67.73; H, 5.44; Cl, 8.69; N, 10.30; O, 7.84
|
CAS # |
1346133-08-1
|
Related CAS # |
1346133-08-1
|
Appearance |
Solid powder
|
SMILES |
C1C[C@H](N(C1)CC2=CC=C(C=C2)OC3=C(C=C(C=C3)C(=O)N)Cl)C4=CN=CC=C4
|
InChi Key |
LOOCZNLSXJHWTG-NRFANRHFSA-N
|
InChi Code |
InChI=1S/C23H22ClN3O2/c24-20-13-17(23(25)28)7-10-22(20)29-19-8-5-16(6-9-19)15-27-12-2-4-21(27)18-3-1-11-26-14-18/h1,3,5-11,13-14,21H,2,4,12,15H2,(H2,25,28)/t21-/m0/s1
|
Chemical Name |
3-chloro-4-[4-[[(2S)-2-pyridin-3-ylpyrrolidin-1-yl]methyl]phenoxy]benzamide
|
Synonyms |
LY2795050; LY 2795050; LY-2795050; (S)-LY2795050
|
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)
|
Solubility (In Vitro) |
DMSO: ~50 mg/mL (~122.6 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.13 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 (6.13 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4516 mL | 12.2582 mL | 24.5164 mL | |
5 mM | 0.4903 mL | 2.4516 mL | 4.9033 mL | |
10 mM | 0.2452 mL | 1.2258 mL | 2.4516 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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05547542 | Recruiting | Drug: CVL-354 Drug: [11C]-LY2795050 |
Opioid Use Disorder | Cerevel Therapeutics, LLC | March 1, 2023 | Phase 1 |
PET images of [11C]LY2795050 in transverse (left column), coronal (middle column) and saggital view (right column). J Nucl Med . 2013 Mar;54(3):455-63. td> |
Left panel: time-activity curves (TACs) in the monkey brain regions following administration of [11C]LY2795050. J Nucl Med . 2013 Mar;54(3):455-63. td> |