Mefloquine hydrochloride

Modify Date: 2024-01-02 21:55:21

Mefloquine hydrochloride Structure
Mefloquine hydrochloride structure
 Common Name Mefloquine hydrochloride
CAS Number 51773-92-3 Molecular Weight 378.312
Density 1.4±0.1 g/cm3 Boiling Point 415.7±40.0 °C at 760 mmHg
Molecular Formula C17H17ClF6N2O Melting Point 250-254ºC
MSDS Chinese USA Flash Point 205.2±27.3 °C
Symbol GHS07
GHS07		 Signal Word Warning

 Use of Mefloquine hydrochloride


Mefloquine hydrochloride is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. IC50 Value: 1 microM ( for K+ channel) [1]Target: AntiparasiticMefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. MQ can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cells [2].in vitro: Mefloquine inhibitedKvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Block of HERG displayed a positive voltage dependence with maximal inhibition obtained at more depolarized potentials [1]. MQ has a highly selective cytotoxicity that inhibits PCa cell growth. MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells [2]. in vivo: Pregnant rats were treated orally with AS (15 and 40 mg/kg body weight (bwt)/day), MQ (30 and 80 mg/kg bwt/day) and AS/MQ (15/30 and 40/80 mg/kg bwt/day) on days 9-11 post coitum (pc). The dams were euthanized on day 12 pc and gestational and embryos histological parameters were evaluated [3].Clinical trial: Activity of Mefloquine Against Urinary Schistosomiasis . Phase 2

 Names

Name Mefloquine Hydrochloride
Synonym More Synonyms

 Mefloquine hydrochloride Biological Activity

Description Mefloquine hydrochloride is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. IC50 Value: 1 microM ( for K+ channel) [1]Target: AntiparasiticMefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. MQ can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cells [2].in vitro: Mefloquine inhibitedKvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Block of HERG displayed a positive voltage dependence with maximal inhibition obtained at more depolarized potentials [1]. MQ has a highly selective cytotoxicity that inhibits PCa cell growth. MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells [2]. in vivo: Pregnant rats were treated orally with AS (15 and 40 mg/kg body weight (bwt)/day), MQ (30 and 80 mg/kg bwt/day) and AS/MQ (15/30 and 40/80 mg/kg bwt/day) on days 9-11 post coitum (pc). The dams were euthanized on day 12 pc and gestational and embryos histological parameters were evaluated [3].Clinical trial: Activity of Mefloquine Against Urinary Schistosomiasis . Phase 2
Related Catalog
References

[1]. Kang J, Chen XL, Wang L, Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK andHERG. J Pharmacol Exp Ther. 2001 Oct;299(1):290-6.

[2]. Yan KH, Yao CJ, Hsiao CH, Mefloquine exerts anticancer activity in prostate cancer cells via ROS-mediated modulation of Akt, ERK, JNK and AMPK signaling. Oncol Lett. 2013 May;5(5):1541-1545.

[3]. Boareto AC, Müller JC, Louren?o EL, Effects of the combined artesunate and mefloquine antimalarial drugs on rat embryos. Hum Exp Toxicol. 2013 Feb 19. [Epub ahead of print]

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 415.7±40.0 °C at 760 mmHg
Melting Point 250-254ºC
Molecular Formula C17H17ClF6N2O
Molecular Weight 378.312
Flash Point 205.2±27.3 °C
Exact Mass 378.116669
PSA 45.15000
LogP 2.87
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.519
Storage condition Refrigerator
Water Solubility DMSO: 38 mg/mL, soluble

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VC0308000
CHEMICAL NAME :
4-Quinolinemethanol, 2,8-bis(trifluoromethyl)-alpha-2-piperidinyl-, monohydrochloride, (R*,S*)-, (+-)-
CAS REGISTRY NUMBER :
51773-92-3
LAST UPDATED :
199603
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C17-H16-F6-N2-O.Cl-H
MOLECULAR WEIGHT :
414.81
WISWESSER LINE NOTATION :
T66 BNJ CXFFF EYQ- BT6MTJ& JXFFF &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
96 mg/kg/52D-I
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Behavioral - excitement Behavioral - aggression
REFERENCE :
AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 154,2360,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
15 mg/kg/3W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma
REFERENCE :
MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 161,453,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
11 mg/kg/2W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 114,994,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
18 mg/kg/5W-I
TOXIC EFFECTS :
Peripheral Nerve and Sensation - paresthesis Behavioral - general anesthetic
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 117,1058,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
880 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
130 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
RIDADR UN 3077 9 / PGIII
WGK Germany 3
RTECS VC0308000

 Articles43

More Articles
Preliminary investigation of the contribution of CYP2A6, CYP2B6, and UGT1A9 polymorphisms on artesunate-mefloquine treatment response in Burmese patients with Plasmodium falciparum malaria.

Am. J. Trop. Med. Hyg. 91(2) , 361-6, (2014)

CYP2A6, CYP2B6, and UGT1A9 genetic polymorphisms and treatment response after a three-day course of artesunate-mefloquine was investigated in 71 Burmese patients with uncomplicated Plasmodium falcipar...

Studying the effect of chloroquine on sporozoite-induced protection and immune responses in Plasmodium berghei malaria.

Malaria Journal 14 , 130, (2015)

Sporozoite immunization of animals and humans under a chemo-prophylactic cover of chloroquine (CPS-CQ) efficiently induces sterile protection against malaria. In humans, CPS-CQ is strikingly more effi...

Comparison between Flow Cytometry, Microscopy, and Lactate Dehydrogenase-Based Enzyme-Linked Immunosorbent Assay for Plasmodium falciparum Drug Susceptibility Testing under Field Conditions.

J. Clin. Microbiol. 53 , 3296-303, (2015)

Flow cytometry is an objective method for conducting in vitro antimalarial sensitivity assays with increasing potential for application in field sites. We examined in vitro susceptibility to seven ant...

 Synonyms

Mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
EINECS 257-412-0
[2,8-bis(trifluoromethyl)quinolin-4-yl](piperidin-2-yl)methanol
4-quinolinemethanol, a-2-piperidinyl-2,8-bis(trifluoromethyl)-
[2,8-Bis(trifluoromethyl)-4-quinolinyl](2-piperidinyl)methanol
MFCD00797519
(AS)-rel-a-(2R)-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol monohydrochloride
4-Quinolinemethanol, α-2-piperidinyl-2,8-bis(trifluoromethyl)-
α-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
Mefloquine (hydrochloride)
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