Orphenadrine citrate

Name: Orphenadrine citrate
Brand: MedChemExpress
SKU: HY-B0369A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0369A Purity: 99.41%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a K_i of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.

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

Orphenadrine citrate Chemical Structure

CAS No. : 4682-36-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 27	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 27	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 25	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Orphenadrine citrate:

Orphenadrine-d₃ citrate Get quote
Orphenadrine Get quote
Orphenadrine hydrochloride Get quote
Orphenadrine citrate (Standard) Get quote

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AMPA Receptor NMDA Receptor Kainate Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

NMDA Receptor

6 μM (Ki)

In Vitro

Orphenadrine citrate (12 μM; 24.5 h) shows neuroprotective effects on 3-NPA-induced neurotoxicity cerebellar granule cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	CGC cells (7-day-old Sprague Dawley rat)
Concentration:	6, 12, 24, 48 µM
Incubation Time:	24.5 h
Result:	Prevented cells from 3-NPA induced cellular aggregation,volume diminution and neurite fragmentation.

In Vivo

Orphenadrine citrate (10, 20, 30 mg/kg; i.p.; once aday for 3 days) reduces 3-NPA-induced mortality in a dose-dependent manner^[1].
Orphenadrine citrate (30 mg/kg; i.p.; once aday for 3 days) shows activity to against 3-NPA-induced neuronal damage in vivo^[1].

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

Animal Model:	Adult male Sprague Dawley rats (275-300 g; 3-NPA toxicity model)^[1].
Dosage:	10, 20, 30 mg/kg
Administration:	Intraperitoneal injection; once aday for 3 days (30 min before 3-NPA).
Result:	Reduced mortality of 3-NPA toxicity rats to 10-40% (3-NPA-treated animals showed general incoordination, drowsiness and general weakness). Recovered 3-NPA-induced body weight loss, and when at 30 mg/kg reduced the level of PBR and expression of HSP27. (PBR and HSP27 are markers of neuronal damage).

Clinical Trial

Molecular Weight

461.50

Formula

C₂₄H₃₁NO₈

CAS No.

4682-36-4

Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C.O=C(CC(C(O)=O)(O)CC(O)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (216.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 10 mg/mL (21.67 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1668 mL	10.8342 mL	21.6685 mL
5 mM	0.4334 mL	2.1668 mL	4.3337 mL
10 mM	0.2167 mL	1.0834 mL	2.1668 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 and light). 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)

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: ≥ 2.5 mg/mL (5.42 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 (5.42 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 36.67 mg/mL (79.46 mM); Clear solution; Need ultrasonic

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 and light)

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: 99.41%

Select Batch:

Data Sheet (278 KB) SDS (479 KB)

COA (254 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Pubill D, et al. Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. Br J Pharmacol. 2001 Feb;132(3):693-702. [Content Brief]

[2]. Kornhuber J, et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.1668 mL	10.8342 mL	21.6685 mL	54.1712 mL
	5 mM	0.4334 mL	2.1668 mL	4.3337 mL	10.8342 mL
	10 mM	0.2167 mL	1.0834 mL	2.1668 mL	5.4171 mL
	15 mM	0.1445 mL	0.7223 mL	1.4446 mL	3.6114 mL
	20 mM	0.1083 mL	0.5417 mL	1.0834 mL	2.7086 mL
DMSO	25 mM	0.0867 mL	0.4334 mL	0.8667 mL	2.1668 mL
	30 mM	0.0722 mL	0.3611 mL	0.7223 mL	1.8057 mL
	40 mM	0.0542 mL	0.2709 mL	0.5417 mL	1.3543 mL
	50 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0834 mL
	60 mM	0.0361 mL	0.1806 mL	0.3611 mL	0.9029 mL
	80 mM	0.0271 mL	0.1354 mL	0.2709 mL	0.6771 mL
	100 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5417 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.