Latanoprostene bunod
Based on 1 Customer Validation
Latanoprostene bunod (NCX116; LBN) is a nitric oxide-releasing prostaglandin F2α analog. Latanoprostene bunod is a prodrug that, upon instillation into the eye, is hydrolyzed by corneal esterases into two active metabolites: Latanoprost (HY-B0577) and NO. Latanoprost activates the prostaglandin FP receptor to increase the outflow of aqueous humor through the uveoscleral pathway. NO increases aqueous humor drainage through the trabecular meshwork pathway, achieving synergistic enhancement targeting the dual pathways of aqueous humor outflow. Latanoprostene bunod can be used in research related to open-angle glaucoma and ocular hypertension.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.75%
- CAS. Nr.: 860005-21-6
- Formel: C27H41NO8
- Molecular Weight:507.62
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Latanoprostene bunod (1.5 μM) increases cGMP levels with an EC50 of 1.5 μM and reduces cytoskeletal contractility and cell resistance in human trabecular meshwork cells[2].
Latanoprostene bunod is rapidly hydrolysed in rabbit and primate corneal homogenate with half-lives of 0.05 min and 0.40 min, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Latanoprostene bunod exhibits IOP-lowering activity in F-prostanoid receptor knockout mice, indicating this effect is mediated by nitric oxide action on the trabecular meshwork pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 860005-21-6
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Appearance Oil
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Molecular Weight 507.62
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Formel C27H41NO8
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Color Colorless to light yellow
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SMILES
O=C(OCCCCO[N+]([O-])=O)CCC/C=C\C[C@@H]1[C@@H](CC[C@@H](O)CCC2=CC=CC=C2)[C@H](O)C[C@@H]1O
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Synonyms
NCX116; LBN
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (197.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9700 mL | 9.8499 mL | 19.6998 mL | 49.2494 mL |
| 5 mM | 0.3940 mL | 1.9700 mL | 3.9400 mL | 9.8499 mL | |
| 10 mM | 0.1970 mL | 0.9850 mL | 1.9700 mL | 4.9249 mL | |
| 15 mM | 0.1313 mL | 0.6567 mL | 1.3133 mL | 3.2833 mL | |
| 20 mM | 0.0985 mL | 0.4925 mL | 0.9850 mL | 2.4625 mL | |
| 25 mM | 0.0788 mL | 0.3940 mL | 0.7880 mL | 1.9700 mL | |
| 30 mM | 0.0657 mL | 0.3283 mL | 0.6567 mL | 1.6416 mL | |
| 40 mM | 0.0492 mL | 0.2462 mL | 0.4925 mL | 1.2312 mL | |
| 50 mM | 0.0394 mL | 0.1970 mL | 0.3940 mL | 0.9850 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3283 mL | 0.8208 mL | |
| 80 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6156 mL | |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4925 mL |
- Latanoprostene bunod
- 860005-21-6
- NCX116
- LBN
- NCX 116
- NCX-116
- Prostaglandin Receptor
- open-angle glaucoma
- matrix metalloproteinase enzymes
- uveoscleral pathways
- prostaglandin F receptor
- Rho-kinase
- Rho pathways
- Schlemm’s canal cells
- trabecular meshwork pathways
- soluble guanylyl cyclase/cyclic guanosine monophosphate signaling
- aqueous humor
- Inhibitor
- inhibitor
- inhibit