2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. L-765314

L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.

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L-765314

L-765314 構造式

CAS 番号 : 189349-50-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 63 在庫あり
Solution
10 mM * 1 mL in DMSO USD 63 在庫あり
Solid
5 mg $55 在庫あり
10 mg $85 在庫あり
25 mg $170 在庫あり
50 mg $270 在庫あり
100 mg $400 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of L-765314:

L-765314 関連抗体

Top Publications Citing Use of Products

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

すべてのアイソフォームを表示
α adrenergic receptor β adrenergic receptor

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  • 純度とドキュメンテーション

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製品説明

L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.

IC50 & Target

Ki: 5.4 nM (rat α1b receptor ), 2.0 nM (human α1b receptor), 50 (rat α1d receptor), 34 nM (human α1d receptor), 500 nM (rat α1a receptor ), 420 nM (human α1a receptor)[1].
体外実験

L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC50) 1.90 nM and represents binding to the R1b sites. The low-affinity site accounts for the residual 75% of binding (IC50) 790 nM and represents binding to the R1a sites[1].

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

L-765314 関連抗体
体内実験

The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean Cmax of L-765314 (A322312) is 1.05 μM and the t1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD25>3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv)[1].

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

522.60

分子式

C27H34N6O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@H](C(NC(C)(C)C)=O)CN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)OCC4=CC=CC=C4
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 : 50 mg/mL (95.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9135 mL 9.5675 mL 19.1351 mL
5 mM 0.3827 mL 1.9135 mL 3.8270 mL
10 mM 0.1914 mL 0.9568 mL 1.9135 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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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 (4.78 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 (4.78 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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mg/kg

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g

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(per animal)

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Number of animals

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: 99.92%

COA (249 KB) HNMR (271 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[1]

Rats[1]
The potency of terazosin and L-765314 for inhibiting the pressor responses to phenylephrine and A-61603 is evaluated in anesthetized male Sprague-Dawley rats (n=4). The rats are dosed i.v with either vehicle or ascending doses of test compounds, and the peak changes in mean arterial pressure are measured. The dose of antagonist eliciting a 25 mmHg decrease in mean arterial pressure (AD25) is calculated as an index of hypotensive potency. The rats are dosed i.v with L-765314 at 3 mg/kg , and the plasma is assayed by LCMS for parent compound[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 1.9135 mL 9.5675 mL 19.1351 mL 47.8377 mL
5 mM 0.3827 mL 1.9135 mL 3.8270 mL 9.5675 mL
10 mM 0.1914 mL 0.9568 mL 1.9135 mL 4.7838 mL
15 mM 0.1276 mL 0.6378 mL 1.2757 mL 3.1892 mL
20 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3919 mL
25 mM 0.0765 mL 0.3827 mL 0.7654 mL 1.9135 mL
30 mM 0.0638 mL 0.3189 mL 0.6378 mL 1.5946 mL
40 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1959 mL
50 mM 0.0383 mL 0.1914 mL 0.3827 mL 0.9568 mL
60 mM 0.0319 mL 0.1595 mL 0.3189 mL 0.7973 mL
80 mM 0.0239 mL 0.1196 mL 0.2392 mL 0.5980 mL
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L-765314 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

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

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

L-765314189349-50-6L765314L 765314Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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製品名:
L-765314
製品番号:
HY-101385
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