Cat. No.: HY-B1052

Lofexidine hydrochloride

(Synonyms: Baq-168; MDL-14042)

Customer Review

Based on 1 Customer Validation

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.

Purity: 99.72%
CAS No.: 21498-08-8
Formula: C₁₁H₁₃Cl₃N₂O
Molecular Weight:295.59

Storage:

4°C, sealed storage, away from moisture

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

Lofexidine hydrochloride Chemical Structure

CAS No.: 21498-08-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

α adrenergic receptor

All Adrenergic Receptor Isoforms :

In Vitro

Lofexidine hydrochloride binds to α₂-adrenergic receptors in rat brain cell membranes, with a K_d 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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 21498-08-8
Appearance Solid
Molecular Weight 295.59
Formula C₁₁H₁₃Cl₃N₂O
Color White to off-white
SMILES

CC(C1=NCCN1)OC2=C(Cl)C=CC=C2Cl.[H]Cl
Synonyms

Baq-168; MDL-14042
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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3831 mL

16.9153 mL

33.8306 mL

5 mM

0.6766 mL

3.3831 mL

6.7661 mL

10 mM

0.3383 mL

1.6915 mL

3.3831 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.04 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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Vartak AP, et al. The preclinical discovery of lofexidine for the treatment of opiate addiction. Expert Opin Drug Discov. 2014;9(11):1371-1377. [Content Brief]

[2]. Gish E C, et al. Lofexidine, an α2-receptor agonist for opioid detoxification[J]. Annals of Pharmacotherapy, 2010, 44(2): 343-351.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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