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MedKoo Cat#: 525872 | Name: Dexpramipexole HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Dexpramipexole, also known as KNS-760704, is an orally administered drug candidate shown to selectively and significantly lower eosinophil counts in human blood and tissue. Dexpramipexole is the enantiomer of pramipexole. It is a low molecular weight, orally bioavailable, water-soluble small molecule with linear pharmacokinetics. Dexpramipexole (DPX) easily crosses the blood brain barrier (BBB) and exerts antioxidative properties by reducing ROS production, while the role of DPX in ferroptosis after ICH remains elusive.

Chemical Structure

Dexpramipexole HCl
Dexpramipexole HCl
CAS#104632-27-1 (2HCl)

Theoretical Analysis

MedKoo Cat#: 525872

Name: Dexpramipexole HCl

CAS#: 104632-27-1 (2HCl)

Chemical Formula: C10H19Cl2N3S

Exact Mass: 0.0000

Molecular Weight: 284.24

Elemental Analysis: C, 42.26; H, 6.74; Cl, 24.94; N, 14.78; S, 11.28

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
104632-27-1 (2HCl) 104632-28-2 (free base) 908244-04-2 (2HCl hydrate)
Synonym
Dexpramipexole dihydrochloride; R-Pramipexole; R-(+)-Pramipexole dihydrochloride; RPPX; SND 919CL2X; KNS760704; KNS 760704; KNS-760704;
IUPAC/Chemical Name
(R)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine dihydrochloride
InChi Key
QMNWXHSYPXQFSK-XCUBXKJBSA-N
InChi Code
InChI=1S/C10H17N3S.2ClH/c1-2-5-12-7-3-4-8-9(6-7)14-10(11)13-8;;/h7,12H,2-6H2,1H3,(H2,11,13);2*1H/t7-;;/m1../s1
SMILES Code
CCCN[C@@H]1CCC2=C(C1)SC(N)=N2.Cl.Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Dexpramipexole dihydrochloride ((R)-Pramipexole dihydrochloride) is a neuroprotective agent and weak non-ergoline dopamine agonist.
In vitro activity:
It was first asked whether DEX (dexpramipexole) improves energy dynamics of primary cultures of neural cells. Cultures of pure cortical neurons or glia from mice were therefore exposed to the drug and intracellular ATP concentrations measured by different means. It was found that DEX increased ATP content in both types of cultures (Figure 1A, B). These findings suggested that DEX increases energy production in neural cells by promoting mitochondrial ATP production. To confirm this hypothesis, ATP production was next monitored within mitochondria of living neurons or astrocytes by means of a mitochondrially targeted luciferase as sensor of ongoing mitochondrial ATP synthesis. Again, it was found that preincubation with DEX increased photon emission of transfected neurons or astrocytes (Supporting Information Figure S1). Additionally, DEX reduced ATP loss in mixed cortical cell cultures exposed to in vitro ischaemia. The drug also improved energy recovery upon re‐exposure of cultures to nutrients and normoxia (Figure 1E). Consistent with the effects of DEX on mitochondrial bioenergetics, it was found that the drug reduced both the extent of intracellular Ca2+ increase and the number of cells undergoing DCD in cultured primary neurons exposed to OGD (Figure 1F–H). Importantly, in keeping with the causative role of DCD in ischaemic neurodegeneration, DEX reduced cell death of both primary neuronal or glial cultures exposed to OGD (Supporting Information Figure S3). Reference: Br J Pharmacol. 2018 Jan; 175(2): 272–283. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5758384/
In vivo activity:
The effects of dexpramipexole on infarct volumes and neurological functions were evaluated in mice following proximal or distal middle cerebral artery occlusion (MCAo). As shown in Figure 4A–C, DEX administered twice daily starting at reperfusion reduced ischaemic brain injury in mice subjected to tMCAo. To confirm the ability of DEX to support mitochondrial bioenergetics, ATP content was anaylzyed within the ischaemic penumbra early (3 h) after reperfusion. Data shown in Figure 4D indicate that energy content of the ischaemic brain tissue was higher in mice treated with DEX. The same dosing was then prolonged up to 7 days and evaluated neuroscore of tMCAo mice for 1 month. Remarkably, DEX provided functional neuroprotection, leading to significant recovery of sensorimotor functions (Figure 4E, F). It was also found that DEX reduced injury of permanent brain ischaemia when treatment started either immediately or even 1 h after artery cauterization (Figure 4L, M). Remarkably, the drug afforded ischaemic neuroprotection even in rats subjected to permanent brain ischaemia (Figure 4N–P), thereby indicating that DEX‐dependent ischaemic neuroprotection in vivo is not species specific. Reference: Br J Pharmacol. 2018 Jan; 175(2): 272–283. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5758384/
Solvent mg/mL mM
Solubility
DMSO 53.0 186.46
H2O 100.0 351.81
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 284.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Muzzi M, Gerace E, Buonvicino D, Coppi E, Resta F, Formentini L, Zecchi R, Tigli L, Guasti D, Ferri M, Camaioni E, Masi A, Pellegrini-Giampietro DE, Mannaioni G, Bani D, Pugliese AM, Chiarugi A. Dexpramipexole improves bioenergetics and outcome in experimental stroke. Br J Pharmacol. 2018 Jan;175(2):272-283. doi: 10.1111/bph.13790. Epub 2017 May 12. PMID: 28320070; PMCID: PMC5758384. 2. Buonvicino D, Ranieri G, Pratesi S, Gerace E, Muzzi M, Guasti D, Tofani L, Chiarugi A. Neuroprotection induced by dexpramipexole delays disease progression in a mouse model of progressive multiple sclerosis. Br J Pharmacol. 2020 Jul;177(14):3342-3356. doi: 10.1111/bph.15058. Epub 2020 Apr 18. PMID: 32199028; PMCID: PMC7312322.
In vitro protocol:
1. Muzzi M, Gerace E, Buonvicino D, Coppi E, Resta F, Formentini L, Zecchi R, Tigli L, Guasti D, Ferri M, Camaioni E, Masi A, Pellegrini-Giampietro DE, Mannaioni G, Bani D, Pugliese AM, Chiarugi A. Dexpramipexole improves bioenergetics and outcome in experimental stroke. Br J Pharmacol. 2018 Jan;175(2):272-283. doi: 10.1111/bph.13790. Epub 2017 May 12. PMID: 28320070; PMCID: PMC5758384. 2. Buonvicino D, Ranieri G, Pratesi S, Gerace E, Muzzi M, Guasti D, Tofani L, Chiarugi A. Neuroprotection induced by dexpramipexole delays disease progression in a mouse model of progressive multiple sclerosis. Br J Pharmacol. 2020 Jul;177(14):3342-3356. doi: 10.1111/bph.15058. Epub 2020 Apr 18. PMID: 32199028; PMCID: PMC7312322.
In vivo protocol:
1. Muzzi M, Gerace E, Buonvicino D, Coppi E, Resta F, Formentini L, Zecchi R, Tigli L, Guasti D, Ferri M, Camaioni E, Masi A, Pellegrini-Giampietro DE, Mannaioni G, Bani D, Pugliese AM, Chiarugi A. Dexpramipexole improves bioenergetics and outcome in experimental stroke. Br J Pharmacol. 2018 Jan;175(2):272-283. doi: 10.1111/bph.13790. Epub 2017 May 12. PMID: 28320070; PMCID: PMC5758384. 2. Buonvicino D, Ranieri G, Pratesi S, Gerace E, Muzzi M, Guasti D, Tofani L, Chiarugi A. Neuroprotection induced by dexpramipexole delays disease progression in a mouse model of progressive multiple sclerosis. Br J Pharmacol. 2020 Jul;177(14):3342-3356. doi: 10.1111/bph.15058. Epub 2020 Apr 18. PMID: 32199028; PMCID: PMC7312322.
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