| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
At Kappa opioid receptors, navacaprant (BTRX-335140) (0-10 μM; 4 hours) demonstrates selective antagonist action [1].
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|---|---|
| ln Vivo |
Navacaprant (BTRX-335140) (0.01-3 mg/kg; once oral) lowers plasma prolactin secretion triggered by U69,593 to levels not induced by U69,593 [1]. When administered intraperitoneally, navacaprant (BTRX-335140) (1 mg/kg) inhibits the analgesic action of hot water due to U-50488 [1]. 1.19 BTRX-335140 pharmacokinetic properties in rodents [1]. AUC0-t (h• ng/mL) 153 725 265 232 Vss (L/kg) 13.8 7.72 F (%) 30.2 12 Rat IV 1 mg/kg, Mouse IV 3 mg/kg, Rat PO 5 mg/kg, and Mouse PO 10 mg/kg CL (mL/min/kg) 105 66.5 t1/2 (h) 1.81 1.91 6.19 2.57
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| Cell Assay |
Cell viability assay [1]
Cell Types: OPRK1-BLA U2OS Cell Tested Concentrations: 0-10 μM Incubation Duration: 4 hrs (hours) Experimental Results: demonstrated antagonistic activity against KOR, DOR and MOR, with IC50 values of 0.8, 110 and 6500 nM respectively, and Displays selective antagonistic activity of KOR. |
| Animal Protocol |
Animal/Disease Models: Rat PRL model [1]
Doses: 0.01, 0.03, 0.1, 0.3, 1 and 3 mg /kg Route of Administration: po (oral gavage); 0.01-3 mg/kg Primary Experimental Results:Even at a dose of 0.1 mg/kg, it can effectively reduce the high level of prolactin caused by U69,593. Animal/Disease Models: Adult male ICR mice, tail immersed in 50°C hot water [1] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; 1 mg/kg Primary Experimental Results:Resistance during 1 hour instead of 24 hrs (hrs (hours)) of pretreatment blocked U-50488-induced analgesia and demonstrated drug-like duration of action in blocking KOR. |
| References | |
| Additional Infomation |
BTRX-335140 is under investigation in clinical trial NCT04221230 (Study in Major Depressive Disorder With BTRX-335140 vs Placebo).
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| Molecular Formula |
C25H32FN5O2
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|---|---|
| Molecular Weight |
453.552289009094
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| Exact Mass |
453.254
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| CAS # |
2244614-14-8
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| PubChem CID |
137434175
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC(CC)=CC2=C1N=C(C(C1=NC(C)=NO1)=C2C)N1CCC(CC1)NC1CCOCC1
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| InChi Key |
CQOJHAJWCDJEAT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H32FN5O2/c1-4-17-13-20-15(2)22(25-27-16(3)30-33-25)24(29-23(20)21(26)14-17)31-9-5-18(6-10-31)28-19-7-11-32-12-8-19/h13-14,18-19,28H,4-12H2,1-3H3
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| Chemical Name |
1-[6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl]-N-(oxan-4-yl)piperidin-4-amine
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| Synonyms |
BTRX335140; BTRX 335140; BTRX-335140
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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 : ~3.85 mg/mL (~8.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.68 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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 1 mg/mL (2.20 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.20 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2048 mL | 11.0241 mL | 22.0483 mL | |
| 5 mM | 0.4410 mL | 2.2048 mL | 4.4097 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2048 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.
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