Bradanicline
Based on 1 Customer Validation
Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.
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- Purity: 98.51%
- CAS No.: 639489-84-2
- 화학식: C22H23N3O2
- 분자량:361.44
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
54 μM
Compound: 7a, TC-5619
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Inhibition of human ERG expressed in CHO cells by whole cell voltage clamp assay
Inhibition of human ERG expressed in CHO cells by whole cell voltage clamp assay
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[PMID: 23126648] |
| GH4-C1 | EC50 |
17 nM
Compound: 7a, TC-5619
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Agonist activity at rat alpha7 nAchR expressed in GH4C1 cells by whole cell patch clamp assay
Agonist activity at rat alpha7 nAchR expressed in GH4C1 cells by whole cell patch clamp assay
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[PMID: 23126648] |
Bradanicline (30 mg/kg; i.p.; 30 min prior to challenge) inhibits citric acid-induced cough in male Hartley guinea pigs, but shows no such effect when delivered directly to the airways via aerosol at a concentration of 3 mg/mL (concurrently with citric acid challenge)[1].
Bradanicline (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) inhibits bradykinin-induced cough in male Hartley guinea pigs[1].
Bradanicline (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) inhibits nicotine-induced cough in male Hartley guinea pigs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 639489-84-2
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Appearance Solid
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분자량 361.44
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화학식 C22H23N3O2
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Color White to off-white
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SMILES
O=C(C1=CC2=CC=CC=C2O1)N[C@H]3[C@H](CC4=CC=CN=C4)N5CCC3CC5
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Synonyms
TC-5619
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 25 mg/mL (69.17 mM; ultrasonic and warming and heat to 60°C; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.92 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 (6.92 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.
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 2.7667 mL | 13.8336 mL | 27.6671 mL | 69.1678 mL |
| 5 mM | 0.5533 mL | 2.7667 mL | 5.5334 mL | 13.8336 mL | |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7667 mL | 6.9168 mL | |
| 15 mM | 0.1844 mL | 0.9222 mL | 1.8445 mL | 4.6112 mL | |
| 20 mM | 0.1383 mL | 0.6917 mL | 1.3834 mL | 3.4584 mL | |
| 25 mM | 0.1107 mL | 0.5533 mL | 1.1067 mL | 2.7667 mL | |
| 30 mM | 0.0922 mL | 0.4611 mL | 0.9222 mL | 2.3056 mL | |
| 40 mM | 0.0692 mL | 0.3458 mL | 0.6917 mL | 1.7292 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5533 mL | 1.3834 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4611 mL | 1.1528 mL |
Bradanicline Related Classifications
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