L-771688
Based on 1 Customer Validation
L-771688 is a highly selective α1A-Adrenoceptor antagonist with a Ki of 0.43±0.02 nM.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 200050-59-5
- Formula: C28H33F2N5O5
- Molecular Weight:557.59
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
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α adrenergic receptor |
Specific [3H]L-771688 binding to cloned human α1A-Adrenoceptors is inhibited with high potency by subtype selective compounds, GG818 (Ki=0.026±0.002 nM) and L-771688 (Ki=0.052±0.008 nM) and subtype non-selective α1-adrenoceptor antagonists, prazosin (Ki=0.088±0.0.032 nM) and terazosin (Ki=1.8±0.65 nM). The relative amount of [3H]L-771688 (0.5 nM) binding in various rat tissue membranes is highest in submaxillary gland (9.5 pmol/g tissue), followed by brain (5.8 pmol/g tissue), vas deferens (4.3 pmol/g tissue), kidney (3.4 pmol/g tissue), heart (1.5 pmol/g tissue), urethra (1.1 pmol/g tissue) and prostate (0.88 pmol/g tissue). In contrast, low specific [3H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue), liver (0.44 pmol/g tissue), aorta (0.11 pmol/g tissue) and spleen (0.11 pmol/g tissue)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 200050-59-5
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Appearance Oil
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Molecular Weight 557.59
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Formula C28H33F2N5O5
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Color Colorless to light yellow
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SMILES
O=C(C([C@H](C1=CC=C(F)C(F)=C1)N2C(NCCCN3CCC(C4=NC=CC=C4)CC3)=O)=C(COC)NC2=O)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (179.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (4.48 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 (4.48 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.
Protocol
[3H]L-771688 is prepared by a catalytic reduction of the precursor, L-797429, in the presence of tritium gas followed by preparative high pressure liquid chromatography. Receptor membranes are prepared for [3H]prazosin/[125I]HEAT binding assays. To measure [3H]L-771688 binding, 980 μL of membranes (cloning human α1A or rat tissues) are added to triplicate tubes containing 10 μL of dimethyl sulfoxide (DMSO) (for total binding) or phentolamine (10 μM final concentration, for nonspecific binding) or tested compounds (at the desiring final concentrations) and 10 μL of [3H]L-771688 (0.3 to 0.6 nM final concentration for routine studies and 10 pM to 5 nM for saturation assays). [3H]L-771688 is diluted in DMSO/methanol/water (1:1:2) from stock solution to minimize its loss to the wall of test tubes. The binding reaction is conducted at 25°C for 1 h or various time intervals in the association rate studies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.7934 mL | 8.9672 mL | 17.9343 mL | 44.8358 mL |
| 5 mM | 0.3587 mL | 1.7934 mL | 3.5869 mL | 8.9672 mL | |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL | 4.4836 mL | |
| 15 mM | 0.1196 mL | 0.5978 mL | 1.1956 mL | 2.9891 mL | |
| 20 mM | 0.0897 mL | 0.4484 mL | 0.8967 mL | 2.2418 mL | |
| 25 mM | 0.0717 mL | 0.3587 mL | 0.7174 mL | 1.7934 mL | |
| 30 mM | 0.0598 mL | 0.2989 mL | 0.5978 mL | 1.4945 mL | |
| 40 mM | 0.0448 mL | 0.2242 mL | 0.4484 mL | 1.1209 mL | |
| 50 mM | 0.0359 mL | 0.1793 mL | 0.3587 mL | 0.8967 mL | |
| 60 mM | 0.0299 mL | 0.1495 mL | 0.2989 mL | 0.7473 mL | |
| 80 mM | 0.0224 mL | 0.1121 mL | 0.2242 mL | 0.5604 mL | |
| 100 mM | 0.0179 mL | 0.0897 mL | 0.1793 mL | 0.4484 mL |
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