2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor Imidazoline Receptor
  4. Lofexidine hydrochloride

Lofexidine hydrochloride  (Synonyms: Baq-168; MDL-14042)

Cat. No.: HY-B1052 Purity: 99.72%
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Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal.

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

Lofexidine hydrochloride

Lofexidine hydrochloride Chemical Structure

CAS No. : 21498-08-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Lofexidine hydrochloride:

Lofexidine hydrochloride Related Antibodies

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal[1][2].

IC50 & Target

α adrenergic receptor

 

In Vitro

Lofexidine hydrochloride binds to α2-adrenergic receptors in rat brain cell membranes, with a Kd value of 5.5 nM[1].
Lofexidine hydrochloride induces peripheral vasoconstriction in isolated rabbit ear central artery specimens[1].
Lofexidine hydrochloride attenuates norepinephrine-induced contraction responses of isolated vas deferens specimens in a concentration-dependent manner[1].

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

Lofexidine hydrochloride Related Antibodies
In Vivo

Lofexidine (administered via duodenal route; administered via intrathecal route) hydrochloride induces sustained, predictable hypotension in rats, with more prominent cardiovascular effects observed after intrathecal administration[1].
Lofexidine (Intravenous administration) hydrochloride induces a transient hypertensive response followed by sustained hypotension in dogs and cats, whereas oral administration only causes hypotension[1].
Lofexidine hydrochloride reduces the expression of Fos protein in the locus coeruleus of morphine-addicted mice during opioid withdrawal[1].
Lofexidine (p.o.) hydrochloride induces reversible neurological symptoms in rats and dogs, with an LD50 of 70-147 mg/kg in rats[2].

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

Animal Model: Rats and dogs[2]
Dosage: /
Administration: p.o.; daily; 1 week (chronic)
Result: Caused sedation, ataxia, exophthalmia, hyperexcitability, and convulsions that resolved by day 2.
Found LD50 between 70 and 147 mg/kg in rats.
Caused liver function test elevations that did not exceed the upper normal limit.
Clinical Trial
Molecular Weight

295.59

Formula

C11H13Cl3N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=NCCN1)OC2=C(Cl)C=CC=C2Cl.[H]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: 

H2O : ≥ 100 mg/mL (338.31 mM)

DMSO : 100 mg/mL (338.31 mM; Need ultrasonic; 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 3.3831 mL 16.9153 mL 33.8306 mL
5 mM 0.6766 mL 3.3831 mL 6.7661 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

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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 (7.04 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 (7.04 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (338.31 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.72%

SDS (480 KB)

COA (254 KB) LCMS (110 KB)

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 (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
H2O / DMSO 1 mM 3.3831 mL 16.9153 mL 33.8306 mL 84.5766 mL
5 mM 0.6766 mL 3.3831 mL 6.7661 mL 16.9153 mL
10 mM 0.3383 mL 1.6915 mL 3.3831 mL 8.4577 mL
15 mM 0.2255 mL 1.1277 mL 2.2554 mL 5.6384 mL
20 mM 0.1692 mL 0.8458 mL 1.6915 mL 4.2288 mL
25 mM 0.1353 mL 0.6766 mL 1.3532 mL 3.3831 mL
30 mM 0.1128 mL 0.5638 mL 1.1277 mL 2.8192 mL
40 mM 0.0846 mL 0.4229 mL 0.8458 mL 2.1144 mL
50 mM 0.0677 mL 0.3383 mL 0.6766 mL 1.6915 mL
60 mM 0.0564 mL 0.2819 mL 0.5638 mL 1.4096 mL
80 mM 0.0423 mL 0.2114 mL 0.4229 mL 1.0572 mL
100 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8458 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Lofexidine hydrochloride Related Classifications

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:

Lofexidine21498-08-8Baq-168 MDL-14042Baq168Baq 168MDL14042MDL 14042MDL-14042Adrenergic ReceptorImidazoline ReceptorBeta Receptoropioid withdrawalc-fosopiate withdrawalopioid dependenceimidazoline I1 receptorlocus coeruleusα2A-adrenergic receptorsopiate dependenceopiate addictionInhibitorinhibitorinhibit

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