1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. L755507

L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM. L755507 enhances the homology-directed repair (HDR)-mediated genome editing.

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L755507

L755507 構造式

CAS 番号 : 159182-43-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 174 在庫あり
Solution
10 mM * 1 mL in DMSO USD 174 在庫あり
Solid
5 mg $135 在庫あり
10 mg $215 在庫あり
25 mg $380 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

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Adrenergic Receptor アイソフォーム固有の製品をすべて表示:

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製品説明

L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM. L755507 enhances the homology-directed repair (HDR)-mediated genome editing[1][2][3].

IC50 & Target

IC50: 35 nM (β3-AR)[1]

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.02 μM
Compound: L-755507
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
[PMID: 11311069]
CHO EC50
0.33 μM
Compound: L-755507
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
[PMID: 11311069]
CHO IC50
3 μM
Compound: 2, (L-755507)
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
[PMID: 9873681]
CHO IC50
3000 nM
Compound: 2, (L-755507)
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
[PMID: 9873681]
体外実験

L755507 causes a robust concentration-dependent increase in cAMP accumulation (pEC50 values of 8.5 and 12.3, respectively). Maximal cAMP accumulation with zinterol and L755507 is increased after pretreatment with pertussis toxin. In contrast to cAMP, zinterol, L755507 and L748337 increase phosphorylation of extracellular signal-regulated kinase 1/2 (Erk1/2) with very high potency (pEC50 values of 10.9, 11.7 and 11.6)[1]. L755507 and Scr7 do not reduce cell viability significantly. Scr7 does not affect cell cycle distribution in a range of 10 to 200 μM. L755507 significantly decreases the proportion of cells in the G2/M phase at 10 μM or 40 μM and increases the S-phase cells at 10 μM compare with the DMSO-treated cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

584.73

分子式

C30H40N4O6S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(NC(NCCCCCC)=O)C=C1)(NC2=CC=C(CCNC[C@H](O)COC3=CC=C(O)C=C3)C=C2)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (171.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7102 mL 8.5510 mL 17.1019 mL
5 mM 0.3420 mL 1.7102 mL 3.4204 mL
10 mM 0.1710 mL 0.8551 mL 1.7102 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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体積 (開始)

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体内:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.28 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.28 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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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+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 98.89%

参考文献
細胞実験
[1]

The cytosensor microphysiometer is used to measure β3-AR-mediated increases in ECAR . In brief, CHO β3 cells are seeded into 12-mm Transwell inserts at 5×105 cells/cup and left to adhere overnight. On the day of experiment, cells are equilibrated for 2 h, and cumulative concentration-response curves to L755507, zinterol, or L748337 are constructed in paired sister cells with each concentration of drug exposed to cells for 14 min. Results are expressed as a percentage of the maximal response to L755507. In experiments examining the effect of inhibitors, cells are treated for 30 min before stimulation with appropriate drugs. All drugs are diluted in modified RPMI 1640 medium. These results are expressed as a percentage of the maximal response to L755507, zinterol, or L748337 over basal[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7102 mL 8.5510 mL 17.1019 mL 42.7548 mL
5 mM 0.3420 mL 1.7102 mL 3.4204 mL 8.5510 mL
10 mM 0.1710 mL 0.8551 mL 1.7102 mL 4.2755 mL
15 mM 0.1140 mL 0.5701 mL 1.1401 mL 2.8503 mL
20 mM 0.0855 mL 0.4275 mL 0.8551 mL 2.1377 mL
25 mM 0.0684 mL 0.3420 mL 0.6841 mL 1.7102 mL
30 mM 0.0570 mL 0.2850 mL 0.5701 mL 1.4252 mL
40 mM 0.0428 mL 0.2138 mL 0.4275 mL 1.0689 mL
50 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8551 mL
60 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7126 mL
80 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5344 mL
100 mM 0.0171 mL 0.0855 mL 0.1710 mL 0.4275 mL
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  • Dilution Calculator

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
L755507
製品番号:
HY-19334
数量:
MCE 日本正規代理店: