Cat. No.: HY-17355B

Dexpramipexole

(Synonyms: (R)-Pramipexole; R-(+)-Pramipexole; KNS-760704)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Dexpramipexole ((R)-Pramipexole) is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Na_v1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.

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Pureté: 99.56%
CAS No.: 104632-28-2
Formule: C₁₀H₁₇N₃S
Masse moléculaire:211.33

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Dexpramipexole Chemical Structure

CAS No.: 104632-28-2

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[5]^[1]

Na_v1.8

GPX4

PINK1

NLRP3 inflammasome

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase :

GPX1
GPX4

Voir tous les produits spécifiques à Isoform Sodium Channel :

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR) :

In Vitro

Dexpramipexole (5-200 μM; 24 h) shows no cytotoxicity to primary cardiomyocytes isolated from neonatal rats at concentrations below 100 μM, while the compound at 200 μM reduces cell viability^[1].
Dexpramipexole (2-50 μM) protects primary neonatal rat cardiomyocytes against hypoxia/reoxygenation (H/R)-induced injury by enhancing cell viability and reducing LDH release^[1].
Dexpramipexole (2-50 μM) upregulates the expression level of PINK1 protein in primary cardiomyocytes from neonatal rats treated with H/R^[1].
Dexpramipexole protects primary cardiomyocytes from neonatal rats against H/R-induced mitochondrial dysfunction by reducing mPTP opening, decreasing ROS production and restoring mitochondrial membrane potential^[1].
Dexpramipexole enhances ATG7-dependent mitophagy in primary neonatal rat cardiomyocytes subjected to H/R, which is characterized by increased formation of mitophagosomes, enhanced autophagic mitochondrial sequestration, and improved mitochondrial clearance^[1].
Dexpramipexole activates PINK1 and Parkin and promotes mitochondrial fission in primary neonatal rat cardiomyocytes exposed to H/R^[1].
Dexpramipexole protects primary cardiomyocytes from neonatal rats against H/R injury by upregulating PINK1- and Parkin-dependent mitophagy^[1].
Dexpramipexole (10 μM; 5 min) inhibits tetrodotoxin-resistant sodium currents in primary cultured rat dorsal root ganglion neurons with an IC₅₀ of 294.4 nM, and does not alter the voltage-dependent activation or inactivation properties of the channels^[5].
Dexpramipexole (10 μM) selectively inhibits Nav1.8-mediated sodium currents in primary cultured dorsal root ganglion neurons from wild-type mice^[5].

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

In Vivo

Dexpramipexole (1 mg/kg; single administration) alleviates myocardial ischemia/reperfusion injury in male C57BL/6 mice by reducing infarct size, restoring cardiac function, decreasing serum levels of myocardial injury biomarkers, and enhancing PINK1/Parkin-dependent mitophagy^[1].
Dexpramipexole (5-20 mg/kg; i.p., once daily for 14 consecutive days) improves survival rate, body weight gain, spontaneous activity, motor coordination and forelimb muscle strength, reduces hematoma volume, alleviates white matter injury, decreases iron and ROS accumulation, and inhibits ferroptosis by upregulating GPX4 and FSP1 in mice with intracerebral hemorrhage^[2].
Dexpramipexole (3 mg/kg; i.p.; once daily for 6 consecutive days) improves lipopolysaccharide (LPS)-induced cognitive impairment in sepsis-associated encephalopathy (SAE), preserves the morphology and function of hippocampal mitochondria in mice, and inhibits mitochondria-mediated pyroptosis and apoptosis^[3].
Dexpramipexole (3-20 mg/kg; 20-140 μg/20 μL; p.o.; i.p.; hind paw s.c.; single administration) exerts effective analgesic effects in various mouse models of nociceptive pain (e.g., inflammatory pain, visceral pain) and neuropathic pain (e.g., chemotherapy-induced pain, nerve compression pain, diabetic neuropathic pain)^[5].

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

Animal Model:

C57BL/6 (male, 9-10 weeks old, 24-26 g; intracerebral hemorrhage induced by stereotactic injection of autologous tail vein blood)^[2]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

i.p., once daily for 14 days
Result:

Significantly increased the survival rate of mice after cerebral hemorrhage.
Slowed down the postoperative weight loss and promoted the recovery of motor function, motor coordination ability, muscle strength and comprehensive neurological function (BMS).
Reduced iron deposition around the hematoma and the accumulation of reactive oxygen species.
Increased the expression of GPX4 and FSP1.

Animal Model:

C57BL/6 (male, 3 months old, 20-28 g, LPS-induced sepsis-associated encephalopathy)^[3]
Dosage:

3 mg/kg
Administration:

i.p.; daily; 6 consecutive days
Result:

Improved the long-term cognitive dysfunction caused by LPS, particularly spatial working memory and hippocampus-dependent memory.
Protected the mitochondria of hippocampal neurons, improved their morphology (reduced swelling) and function (maintained ATP levels, reduced ROS).
Inhibited pyroptosis and apoptosis of cells

Animal Model:

CD-1 (male, 20-25 g, intraplantar formalin injection-induced inflammatory pain)^[5]
Dosage:

3 mg/kg; 10 mg/kg; 20 μg/20 μL; 70 μg/20 μL; 140 μg/20 μL
Administration:

p.o.; single dose 1 h before test; i.p.; single dose 1 h before test; s.c. in hind paw; single dose 10 min before test
Result:

Reduced time spent in pain-like behaviors during the early formalin phase (10 mg/kg p.o.).
Reduced time spent in pain-like behaviors dose-dependently during the late formalin phase (3 mg/kg, 10 mg/kg p.o.).
Reduced time spent in pain-like behaviors dose-dependently during the late formalin phase (3 mg/kg, 10 mg/kg i.p.).
Reduced time spent in pain-like behaviors during the late formalin phase (70 μg/20 μL, 140 μg/20 μL s.c.).
Caused no effect on pain-like behaviors in the early phase at any tested subdermal dose.

Animal Model:

CD-1 (male, 20-25 g; female, intraperitoneal acetic acid injection-induced visceral pain)^[5]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; single dose 1 h before test
Result:

Reduced the number of abdominal writhings dose-dependently in male mice
. Reduced the number of abdominal writhings in female mice.

Animal Model:

CD-1 (male, 20-25 g, ankle complete Freund adjuvant injection-induced chronic inflammatory arthritis pain)^[5]
Dosage:

70 μg/20 μL
Administration:

s.c. in hind paw; single dose 10 min before each test on day 7, 14, 21
Result:

Increased mechanical thresholds at day 7, 14, and 21 post CFA injection.

Animal Model:

CD-1 (subcutaneous oxaliplatin injection-induced acute chemotherapy-induced neuropathic pain)^[5]
Dosage:

10 mg/kg; 70 μg/20 μL
Administration:

i.p.; single dose 30 min post oxaliplatin; s.c. in hind paw; single dose 50 min post oxaliplatin
Result:

Reduced cold pain-related behaviors at 1, 2, 3, 4, and 5 h post oxaliplatin injection (10 mg/kg i.p.).
Reduced cold pain-related behaviors at 1 hour post oxaliplatin injection (70 μg/20 μL, s.c.).

Animal Model:

CD-1 (intraperitoneal oxaliplatin injection-induced chronic chemotherapy-induced neuropathic pain)^[5]
Dosage:

10 mg/kg
Administration:

i.p.; single dose 1 h before test; p.o.; single dose 1 h before test
Result:

Reduced cold allodynia at day 21 post initial oxaliplatin injection (10 mg/kg i.p.).
Reduced cold allodynia at 1, 3, and 6 hours post dosing, with effects diminishing by 9 hours (10 mg/kg p.o.).

Animal Model:

CD-1 (male, 20-25 g, chronic constriction injury of right sciatic nerve-induced neuropathic pain)^[5]
Dosage:

10 mg/kg
Administration:

i.p.; single dose 1 h before test
Result:

Reduced mechanical allodynia in the injured hind paw.

Animal Model:

CD-1 (intraperitoneal streptozotocin injection-induced diabetic neuropathic pain, blood glucose > 250 mg/dl confirmed 3 weeks post-injection)^[5]
Dosage:

10 mg/kg
Administration:

i.p.; single dose 1 h before test
Result:

Increased latency to pain-related behaviors in diabetic mice.

Chemical Information

CAS No. 104632-28-2
Appearance Solid
Masse moléculaire 211.33
Formule C₁₀H₁₇N₃S
Color White to off-white
SMILES

NC1=NC(CC[C@@H](NCCC)C2)=C2S1
Synonyms

(R)-Pramipexole; R-(+)-Pramipexole; KNS-760704
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Neuroreport

Dexpramipexole ameliorates cognitive deficits in sepsis-associated encephalopathy through suppressing mitochondria-mediated pyroptosis and apoptosis. [Abstract]

2023 Mar 1;34(4):220-231. PMID: 36719835

Dexpramipexole purchased from MedChemExpress. Usage Cited in: Neuroreport. 2023 Mar 1;34(4):220-231. [Abstract]

Dexpramipexole (DPX; 3 mg/kg; i.p.; once daily for 6 consecutive days) attenuates the LPS-induced increase in the number of TUNEL-positive cells in the hippocampus in SAE mice.

Dexpramipexole purchased from MedChemExpress. Usage Cited in: Neuroreport. 2023 Mar 1;34(4):220-231. [Abstract]

Dexpramipexole (DPX; 3 mg/kg; i.p.; once daily for 6 consecutive days) attenuates LPS-induced activation of microglia and astrocytes in the hippocampus in SAE mice. (a) Representative images of Iba-1 staining and quantification of Iba-1 (green) fluorescence intensity in the hippocampal CA1 and DG regions. (b) Representative images of GFAP staining and quantification of GFAP (red) fluorescence intensity in the hippocampal CA1 and DG regions. DAPI staining is shown in blue.
Oxid Med Cell Longev

Dexpramipexole Attenuates White Matter Injury to Facilitate Locomotion and Motor Coordination Recovery via Reducing Ferroptosis after Intracerebral Hemorrhage. [Abstract]

2022 Aug 4;2022:6160701. PMID: 35965685

Solvant et solubilité

In Vitro:

DMSO : 10 mg/mL (47.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

4.7319 mL

23.6597 mL

47.3194 mL

5 mM

0.9464 mL

4.7319 mL

9.4639 mL

10 mM

0.4732 mL

2.3660 mL

4.7319 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 1 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Tang L, et al. Dexpramipexole attenuates myocardial ischemia/reperfusion injury through upregulation of mitophagy. Eur J Pharmacol. 2021;899:173962. [Content Brief]

[2]. Wang B, et al. Dexpramipexole Attenuates White Matter Injury to Facilitate Locomotion and Motor Coordination Recovery via Reducing Ferroptosis after Intracerebral Hemorrhage. Oxid Med Cell Longev. 2022;2022:6160701. Published 2022 Aug 4. [Content Brief]

[3]. Zhang Y, et al. Dexpramipexole ameliorates cognitive deficits in sepsis-associated encephalopathy through suppressing mitochondria-mediated pyroptosis and apoptosis. Neuroreport. 2023;34(4):220-231. [Content Brief]

[4]. Cusack RP, Sulaiman I, Gauvreau GM. Refashioning dexpramipexole: A new horizon in eosinophilic asthma? J Allergy Clin Immunol. 2023 Nov;152(5):1092-1094.
[Content Brief]

[5]. Urru M, et al. Dexpramipexole blocks Nav1.8 sodium channels and provides analgesia in multiple nociceptive and neuropathic pain models. Pain. 2020 Apr;161(4):831-841.
[Content Brief]

[6]. Panch SR, et al. Dexpramipexole as an oral steroid-sparing agent in hypereosinophilic syndromes. Blood. 2018;132(5):501-509. [Content Brief]

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	4.7319 mL	23.6597 mL	47.3194 mL	118.2984 mL
	5 mM	0.9464 mL	4.7319 mL	9.4639 mL	23.6597 mL
	10 mM	0.4732 mL	2.3660 mL	4.7319 mL	11.8298 mL
	15 mM	0.3155 mL	1.5773 mL	3.1546 mL	7.8866 mL
	20 mM	0.2366 mL	1.1830 mL	2.3660 mL	5.9149 mL
	25 mM	0.1893 mL	0.9464 mL	1.8928 mL	4.7319 mL
	30 mM	0.1577 mL	0.7887 mL	1.5773 mL	3.9433 mL
	40 mM	0.1183 mL	0.5915 mL	1.1830 mL	2.9575 mL

Dexpramipexole

2 Cited Publications

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Dexpramipexole

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

NF-κB Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) Dexpramipexole

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase

Voir tous les produits spécifiques à Isoform Sodium Channel

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR)

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Dexpramipexole Related Classifications

HY-17355B Related Classifications