Dexpramipexole dihydrochloride
Based on 2 publication(s) in Google Scholar
Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride 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 dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 104632-27-1
- Formula: C10H19Cl2N3S
- Molecular Weight:284.26
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Dexpramipexole dihydrochloride
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Biological Activity
Dexpramipexole (5-200 μM; 24 h) dihydrochloride 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) dihydrochloride 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) dihydrochloride upregulates the expression level of PINK1 protein in primary cardiomyocytes from neonatal rats treated with H/R[1].
Dexpramipexole dihydrochloride 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 dihydrochloride 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 dihydrochloride activates PINK1 and Parkin and promotes mitochondrial fission in primary neonatal rat cardiomyocytes exposed to H/R[1].
Dexpramipexole dihydrochloride protects primary cardiomyocytes from neonatal rats against H/R injury by upregulating PINK1- and Parkin-dependent mitophagy[1].
Dexpramipexole (10 μM; 5 min) dihydrochloride 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) dihydrochloride 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.
Dexpramipexole (5-20 mg/kg; i.p., once daily for 14 consecutive days) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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.
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Animal Model:C57BL/6 (male, 9-10 weeks old, 24-26 g; intracerebral hemorrhage induced by stereotactic injection of autologous tail vein blood)[2]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p., once daily for 14 days
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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.
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Animal Model:C57BL/6 (male, 3 months old, 20-28 g, LPS-induced sepsis-associated encephalopathy)[3]
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Dosage:3 mg/kg
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Administration:i.p., once daily for 6 days
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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
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Animal Model:CD-1 (male, 20-25 g, intraplantar formalin injection-induced inflammatory pain)[5]
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Dosage:3 mg/kg; 10 mg/kg; 20 μg/20 μL; 70 μg/20 μL; 140 μg/20 μL
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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
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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.
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Animal Model:CD-1 (male, 20-25 g; female, intraperitoneal acetic acid injection-induced visceral pain)[5]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; single dose 1 h before test
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Result:Reduced the number of abdominal writhings dose-dependently in male mice
. Reduced the number of abdominal writhings in female mice.
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Animal Model:CD-1 (male, 20-25 g, ankle complete Freund adjuvant injection-induced chronic inflammatory arthritis pain)[5]
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Dosage:70 μg/20 μL
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Administration:s.c. in hind paw; single dose 10 min before each test on day 7, 14, 21
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Result:Increased mechanical thresholds at day 7, 14, and 21 post CFA injection.
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Animal Model:CD-1 (subcutaneous oxaliplatin injection-induced acute chemotherapy-induced neuropathic pain)[5]
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Dosage:10 mg/kg; 70 μg/20 μL
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Administration:i.p.; single dose 30 min post oxaliplatin; s.c. in hind paw; single dose 50 min post oxaliplatin
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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.).
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Animal Model:CD-1 (intraperitoneal oxaliplatin injection-induced chronic chemotherapy-induced neuropathic pain)[5]
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Dosage:10 mg/kg
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Administration:i.p.; single dose 1 h before test; p.o.; single dose 1 h before test
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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.).
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Animal Model:CD-1 (male, 20-25 g, chronic constriction injury of right sciatic nerve-induced neuropathic pain)[5]
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Dosage:10 mg/kg
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Administration:i.p.; single dose 1 h before test
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Result:Reduced mechanical allodynia in the injured hind paw.
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Animal Model:CD-1 (intraperitoneal streptozotocin injection-induced diabetic neuropathic pain, blood glucose > 250 mg/dl confirmed 3 weeks post-injection)[5]
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Dosage:10 mg/kg
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Administration:i.p.; single dose 1 h before test
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Result:Increased latency to pain-related behaviors in diabetic mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 104632-27-1
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Appearance Solid
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Molecular Weight 284.26
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Formula C10H19Cl2N3S
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Color White to off-white
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SMILES
NC(S1)=NC2=C1C[C@H](NCCC)CC2.[H]Cl.[H]Cl
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Synonyms
(R)-Pramipexole dihydrochloride; R-(+)-Pramipexole dihydrochloride; KNS-760704 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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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 dihydrochloride 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 dihydrochloride 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.
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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
Solvent & Solubility
DMSO : ≥ 100 mg/mL (351.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (351.79 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.32 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.32 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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (351.79 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
Purity & Documentation
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Data Sheet (298 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[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]
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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.5179 mL | 17.5895 mL | 35.1791 mL | 87.9477 mL |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | 17.5895 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 mL | 8.7948 mL | |
| 15 mM | 0.2345 mL | 1.1726 mL | 2.3453 mL | 5.8632 mL | |
| 20 mM | 0.1759 mL | 0.8795 mL | 1.7590 mL | 4.3974 mL | |
| 25 mM | 0.1407 mL | 0.7036 mL | 1.4072 mL | 3.5179 mL | |
| 30 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9316 mL | |
| 40 mM | 0.0879 mL | 0.4397 mL | 0.8795 mL | 2.1987 mL | |
| 50 mM | 0.0704 mL | 0.3518 mL | 0.7036 mL | 1.7590 mL | |
| 60 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL | |
| 80 mM | 0.0440 mL | 0.2199 mL | 0.4397 mL | 1.0993 mL | |
| 100 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 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.
Dexpramipexole dihydrochloride Related Classifications
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