2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Befiradol hydrochloride

Befiradol hydrochloride  (Synonyms: NLX-112 hydrochloride; F 13640 hydrochloride)

製品番号: HY-14785A 純度: 99.93%
COA 取扱説明書 Technical Support

Befiradol (NLX-112) hydrochloride is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression.

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Befiradol hydrochloride

Befiradol hydrochloride 構造式

CAS 番号 : 2436760-81-3

容量 価格（税別） 在庫状況 数量
5 mg $460 在庫あり
10 mg $670 在庫あり
25 mg $1100 在庫あり
50 mg $1500 在庫あり
100 mg $2000 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Befiradol hydrochloride 関連抗体

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製品説明

Befiradol (NLX-112) hydrochloride is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression[1].

IC50 & Target

5-HT1A Receptor

 

体外実験

Befiradol (1-30 μM) hydrochloride does not alleviate DAMGO-induced respiratory depression or alter baseline respiratory rhythm in vitro neonatal rat brainstem-spinal cord preparations[1].

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

Befiradol hydrochloride 関連抗体
体内実験

Befiradol (0.6 mg/kg; subcutaneous injection; single bolus) hydrochloride alleviates fentanyl-induced respiratory depression in neonatal rats by significantly increasing respiratory rate, tidal volume and minute ventilation, and exhibits a superior effect compared with the normal saline control group[1].
Befiradol (0.1-0.4 mg/kg; intravenous injection; single bolus) hydrochloride dose-dependently attenuates fentanyl-induced respiratory depression and sedation in adult rats, but also significantly reduces fentanyl-induced analgesic effects at effective doses[1].
Befiradol (0.2 mg/kg; subcutaneous injection; single bolus dose) hydrochloride induces hyperventilation, hyperalgesia and behavioral syndrome in normal adult rats[1].

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

Animal Model: Sprague-Dawley (neonatal, 3 to 4 days after birth)[1]
Dosage: 0.6 mg/kg
Administration: s.c.; single bolus
Result: Increased relative respiratory frequency to 39.2% of control (vs. saline 24.2% of control).
Increased relative tidal volume to 76.1% of control (vs. saline 52.2% of control).
Increased relative minute ventilation to 29.3% of control (vs. saline 12.4% of control).
Alleviated fentanyl-induced respiratory depression over 20 minutes.
Animal Model: Sprague-Dawley (adult male, 290 to 360 g)[1]
Dosage: 0.1, 0.2, 0.4 mg/kg
Administration: i.v.; single bolus
Result: At 0.1 mg/kg, increased relative minute ventilation to 37.4% of control (vs. saline 18.7% of control) and oxygen saturation to 59.5% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted less than 10 minutes.
At 0.2 mg/kg, increased relative minute ventilation to 53.7% of control (vs. saline 18.7% of control) and oxygen saturation to 75.4% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted beyond fentanyl infusion duration.
At 0.4 mg/kg, increased relative minute ventilation to 65.8% of control (vs. saline 18.7% of control) and oxygen saturation to 78.5% (vs. saline 45.7%) 4 minutes post-administration; alleviation lasted beyond fentanyl infusion duration.
At 0.2 mg/kg, reduced duration of analgesia via tail clamping to 28.4 min (vs. saline 52.4 min) and via thermal paw withdrawal to 90.4 min (vs. saline 130.5 min).
At 0.2 mg/kg, reduced duration of fentanyl-induced sedation to 39.8 min (vs. saline 58 min).
分子量

430.32

分子式

C20H23Cl2F2N3O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=C3)(F)CC2.Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (290.48 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 2.3239 mL 11.6193 mL 23.2385 mL
5 mM 0.4648 mL 2.3239 mL 4.6477 mL
10 mM 0.2324 mL 1.1619 mL 2.3239 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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）

C1

×
体積 （開始）

V1

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濃度 （終了）

C2

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体積 （終了）

V2

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: ≥ 2.08 mg/mL (4.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 2.3239 mL 11.6193 mL 23.2385 mL 58.0963 mL
5 mM 0.4648 mL 2.3239 mL 4.6477 mL 11.6193 mL
10 mM 0.2324 mL 1.1619 mL 2.3239 mL 5.8096 mL
15 mM 0.1549 mL 0.7746 mL 1.5492 mL 3.8731 mL
20 mM 0.1162 mL 0.5810 mL 1.1619 mL 2.9048 mL
25 mM 0.0930 mL 0.4648 mL 0.9295 mL 2.3239 mL
30 mM 0.0775 mL 0.3873 mL 0.7746 mL 1.9365 mL
40 mM 0.0581 mL 0.2905 mL 0.5810 mL 1.4524 mL
50 mM 0.0465 mL 0.2324 mL 0.4648 mL 1.1619 mL
60 mM 0.0387 mL 0.1937 mL 0.3873 mL 0.9683 mL
80 mM 0.0290 mL 0.1452 mL 0.2905 mL 0.7262 mL
100 mM 0.0232 mL 0.1162 mL 0.2324 mL 0.5810 mL
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Befiradol hydrochloride 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 *
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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

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
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    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:

Befiradol2436760-81-3NLX-112F 13640NLX112NLX 112F13640F-136405-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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