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

Name: Befiradol hydrochloride
Brand: MedChemExpress
SKU: HY-14785A
Rating: 4.5 (1 reviews)

Cat. No.: HY-14785A Purity: 99.93%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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.

For research use only. We do not sell to patients.

Befiradol hydrochloride Chemical Structure

CAS No. : 2436760-81-3

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Befiradol hydrochloride:

Befiradol In-stock

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT_1A Receptor

In Vitro

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.

In Vivo

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).

Molecular Weight

430.32

Formula

C₂₀H₂₃Cl₂F₂N₃O

CAS No.

2436760-81-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (245 KB) HNMR (277 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Ren J, et al. 5-HT1A receptor agonist Befiradol reduces fentanyl-induced respiratory depression, analgesia, and sedation in rats. Anesthesiology. 2015;122(2):424-434.

Complete Stock Solution Preparation Table

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

Befiradol hydrochloride Related Classifications

Neurological Disease Metabolic Disease

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:

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

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

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

Customer Review

Other Forms of Befiradol hydrochloride:

Befiradol hydrochloride Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Befiradol hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Befiradol hydrochloride Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report