Product Categories

Flupirtine maleate

Flupirtine maleate is the salt form of Flupirtine, which is a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection.

Catalog No.S1334

: Tel: +1-832-582-8158[email protected]

Flupirtine maleate Chemical Structure
Molecular Weight: 420.39

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Flupirtine maleate is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well)

Product Information

Compare DNA/RNA Synthesis Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1166	Cisplatin	<1 mg/mL	60 mg/mL	<1 mg/mL
S1215	Carboplatin	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1149	Gemcitabine HCl (Gemzar)	23 mg/mL	<1 mg/mL	<1 mg/mL
S1491	Fludarabine (Fludara)	<1 mg/mL	57 mg/mL	<1 mg/mL
S1135	Pemetrexed (Alimta)	94 mg/mL	1 mg/mL	<1 mg/mL
S1224	Oxaliplatin (Eloxatin)	<1 mg/mL	14 mg/mL	<1 mg/mL
S1229	Fludarabine Phosphate (Fludara)	6 mg/mL	73 mg/mL	<1 mg/mL
S1214	Bleomycin sulfate	154 mg/mL	153 mg/mL	<1 mg/mL
S2684	CX-5461	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1209	Adrucil(Fluorouracil)	<1 mg/mL	26 mg/mL	<1 mg/mL
S1156	Capecitabine (Xeloda)	6 mg/mL	72 mg/mL	72 mg/mL
S1782	Azacitidine(Vidaza)	<1 mg/mL	49 mg/mL	<1 mg/mL
S1714	Gemcitabine(Gemzar)	<1 mg/mL	15 mg/mL	<1 mg/mL
S1648	Cytarabine	48 mg/mL	1 mg/mL	<1 mg/mL
S1213	Nelarabine (Arranon)	3 mg/mL	60 mg/mL	<1 mg/mL
S1217	Clafen (Cyclophosphamide)	43 mg/mL	52 mg/mL	52 mg/mL
S1302	Ifosfamide	52 mg/mL	52 mg/mL	52 mg/mL
S1221	Dacarbazine (DTIC-Dome)	<1 mg/mL	3 mg/mL	<1 mg/mL
S1334	Flupirtine maleate	<1 mg/mL	84 mg/mL	3 mg/mL
S1384	Mizoribine (Bredinin)	52 mg/mL	1 mg/mL	<1 mg/mL
S2678	NSC-207895 (XI-006)	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1199	Cladribine	<1 mg/mL	57 mg/mL	<1 mg/mL
S1218	Clofarabine	<1 mg/mL	61 mg/mL	<1 mg/mL
S1289	Carmofur	<1 mg/mL	52 mg/mL	10 mg/mL
S1299	Floxuridine (Fludara)	49 mg/mL	49 mg/mL	10 mg/mL
S1305	Mercaptopurine	<1 mg/mL	30 mg/mL	<1 mg/mL
S1192	Raltitrexed (Tomudex)	<1 mg/mL	92 mg/mL	<1 mg/mL
S1300	Ftorafur	8 mg/mL	40 mg/mL	7 mg/mL
S2554	Daphnetin	<1 mg/mL	36 mg/mL	<1 mg/mL
S1981	Adenine	<1 mg/mL	<1 mg/mL	<1 mg/mL
S1983	Adenine HCl	4 mg/mL	8 mg/mL	<1 mg/mL
S1982	Adenine sulfate	2 mg/mL	<1 mg/mL	<1 mg/mL
S1995	Procarbazine HCl (Matulane)	52 mg/mL	<1 mg/mL	52 mg/mL
S2029	Uridine	49 mg/mL	49 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	Flupirtine maleate is the salt form of Flupirtine, which is a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection.
Targets
IC50
In vitro	Flupirtine pre-incubated for 2 hours prevents cell death in rat cortical neurons induced by NMDA and gp120 of HIV-1. ^[1] Flupirtine is capable of protecting primary neurons against glutamate-induced cytotoxicity by reducing calcium ion concentrations at 1-10 mM. ^[2] Flupirtine pretreated for 2 hours preventsβ-amyloid-induced apoptosis in primary neuronal cells at concentrations of 1 or 5μg/mL. ^[3] Flupirtine at concentration of 10 μM markedly decreases nonreceptor-mediated necrotic cell death in PC 12 cultures treated with 10 mM L-glutamate, meanwhile, Flupirtine exerts anti-oxidative effects in PC 12 cultures. ^[4] Flupirtine-maleate at concentrations of 1 μM and 10 μM decreases TRAIL-mediated death of human living brain tissue culture. ^[5] Flupirtine activates inwardly rectifying potassium ion channels and thus stabilizes the resting membrane potential at a therapeutically relevant concentration. ^[6]
In vivo	Pre-treatment with Flupirtine exerts a protective effect on hippocampal and striatal neuronal damage and on deficits in spatial learning in rats with cerebral ischemia. ^[7] Flupirtine administered centrally inhibits the nociceptive responses induced by chemical, thermal, mechanical and electrical stimuli in animal studies. ^[8] Flupirtine exerts muscle relaxant effects in rat. ^[9]
Clinical Trials	Flupirtine has just finished Phase I clinical trials for axonal change, neuronal pain.
Features

Protocol(Only for Reference)

Cell Assay:
^[4]

Cell lines	PC12 cell
Concentrations	1 or 5 μg/mL
Incubation Time	72 hours
Method	For measurement of viability and generation of reactive oxygen intermediates, PC12 cells are seeded in 24- or 96-well plates coated with poly-L-lysine at 10⁵ cells/mL. Drugs are dissolved in PBS (pH 7.4), or ethanol and filtered sterile. At the end of each experiment cells are trypsinized and pelleted together with cells of the culture supernatant. After staining for 10 min with 0.2% Trypan blue solution live (unstained) and dead (Trypan blue positive) cells are counted in a hemocytometer chamber. In addition, cellular viability is evaluated by the reduction of MTT to formazan. After 2 hours incubation with MTT (0.5 mg/ml) at 37 °C, cells are lysed in DMSO. Extinction at 570 nm is determined on a plate photometer. For staining of surviving adherent cells, plates are incubated for 10 min with 0.5% crystalviolet dissolved in 20% methanol. Plates are rinsed with water and stained cells are lysed in 50% ethanol, 0.1 M sodiumcitrate before determining extinction at 550 nm.

Animal Study:
^[7]

Animal Models	male Wistar rats with cerebral ischemia induced by four-vessel-occlusion
Formulation	sterile 0.9% sodium chloride solution
Dosages	5 mg/kg
Administration	Intraperitoneal injection either 20 min before and 50 min after occlusion or directly and 70 min after occlusion

References

Chemical Information

Download Flupirtine maleate SDF

Molecular Weight (MW)	420.39
Formula	C₁₅H₁₇FN₄O₂·C₄H₄O₄
CAS No.	75507-68-5, 56995-20-1 (free base), 33400-45-2 (HCl)
Synonyms	Katadolon

Solubility (25°C) DMSO 84 mg/mL Water <1 mg/mL Ethanol 3 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	Carbamic acid, N-[2-amino-6-[[(4-fluorophenyl)methyl]amino]-3-pyridinyl]-, ethyl ester, (2Z)-2-butenedioate

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related DNA/RNA Synthesis Inhibitors

CCT239065
CCT239065 is a novel and selective BRAF^V600E and LCK inhibitor with IC50 of 13 nM and 6 nM, respectively.
Daphnetin
Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively.
NSC-207895 (XI-006)
NSC-207895 suppresses MDMX with IC50 of 2.5 µM, leading to enhanced p53 stabilization/activation and DNA damage.
CX-5461
CX-5461 selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116 cells.
ABT-888 (Veliparib)

ABT-888 (Veliparib, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM, respectively.
Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.
Iniparib (BSI-201)

BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor.
KU-55933

KU-55933 is a potent and specific ATM inhibitor with IC50 and K_i of 13 nM and 2.2 nM, respectively.
Rucaparib (AG-014699 , PF-01367338)

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM.
INO-1001
INO-1001 is a potent inhibitor of PARP with IC50 of 50 nM and a mediator of oxidant-induced myocyte dysfunction during reperfusion.

Cell Cycle and DNA Damage Related Products

> Download

Choose Your Country or Region

Product Categories

Flupirtine maleate