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Purity: ≥98%
LY-2940094 is a novel, potent, selective and orally bioavailable nociceptin receptor (NOP receptor) antagonist that can be potentially used for the treatment of major depressive disorder and alcoholism. It possesses strong antagonist potency (Kb=0.166 nM) and affinity (Ki=0.105 nM). In animal models, ethanol self-administration is decreased by LY-2940094.
| Targets |
NOP Receptor/ORL1
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|---|---|
| ln Vivo |
LY2940094 (3, 10, or 30 mg/kg; 2-3 mL/kg; side wall daily; for 4 days) Drinking sites reduce alcohol preference in Indiana (P) and Malkigian Sardinia (msP) in large animals Model: Female alcoholic (P) rat (250-320 g); rat, does not affect food/water recognition or locomotor activity [1]. Male Malchigian Sardinian alcohol-preferring (msP) rats (400-450 g) [1] Dosage: 3, 10, or 30 mg/kg; 2-3 mL/kg Administration: Oral; daily; 4-day results: Reduced home cage ethanol self-administration.
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| Animal Protocol |
Female Alcohol-Preferring (P) rats (250-320 g); Male Marchigian Sardinian Alcohol-Preferring (msP) rats (400-450 g)
3, 10, or 30 mg/kg; 2-3 mL/kg Administered orally; daily; 4 days |
| References |
| Molecular Formula |
C22H23CLF2N4O2S
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|---|---|
| Molecular Weight |
480.958429574966
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| Exact Mass |
480.12
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| Elemental Analysis |
C, 54.94; H, 4.82; Cl, 7.37; F, 7.90; N, 11.65; O, 6.65; S, 6.67
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| CAS # |
1307245-86-8
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| Related CAS # |
LY2940094 tartrate; 1307245-87-9
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| Appearance |
Solid powder
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| SMILES |
CC1=NN(C=C1CN2CCC3(CC2)C4=C(C=C(S4)Cl)C(CO3)(F)F)C5=C(C=CC=N5)CO
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| InChi Key |
NKQHBJNRBKHUQR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23ClF2N4O2S/c1-14-16(11-29(27-14)20-15(12-30)3-2-6-26-20)10-28-7-4-21(5-8-28)19-17(9-18(23)32-19)22(24,25)13-31-21/h2-3,6,9,11,30H,4-5,7-8,10,12-13H2,1H3
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| Chemical Name |
[2-[4-[(2-chloro-4,4-difluorospiro[5H-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methylpyrazol-1-yl]pyridin-3-yl]methanol
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| Synonyms |
BTRX 246040; BTRX246040; BTRX-246040; LY-2940094; LY 2940094; LY2940094
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~41.7 mg/mL (~86.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.32 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 20.8 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: ≥ 2.08 mg/mL (4.32 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 20.8 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: ≥ 2.08 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0792 mL | 10.3959 mL | 20.7917 mL | |
| 5 mM | 0.4158 mL | 2.0792 mL | 4.1583 mL | |
| 10 mM | 0.2079 mL | 1.0396 mL | 2.0792 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 |
| NCT01263236 | Completed | Drug: LY2940094 Drug: Placebo |
Major Depressive Disorder | BlackThorn Therapeutics, Inc. | December 2010 | Phase 1 |
| NCT01724112 | Completed | Drug: LY2940094 Drug: Placebo |
Major Depressive Disorder | BlackThorn Therapeutics, Inc. | November 2012 | Phase 2 |
| NCT01404091 | Completed | Drug: LY2940094 | Depression | BlackThorn Therapeutics, Inc. | July 2011 | Phase 1 |
| NCT01798303 | Completed | Drug: LY2940094 Drug: Placebo |
Alcoholism | BlackThorn Therapeutics, Inc. | July 2013 | Phase 2 |
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