Lidoflazine

Modify Date: 2024-01-11 19:58:42

Lidoflazine Structure
Lidoflazine structure
Common Name Lidoflazine
CAS Number 3416-26-0 Molecular Weight 491.61500
Density 1.161g/cm3 Boiling Point 632.6ºC at 760mmHg
Molecular Formula C30H35F2N3O Melting Point 158-162ºC
MSDS Chinese USA Flash Point 336.4ºC

 Use of Lidoflazine


Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K+ channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia[1].

 Names

Name Lidoflazine
Synonym More Synonyms

 Lidoflazine Biological Activity

Description Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K+ channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia[1].
Target

Ca2+

In Vitro Lidoflazine inhibits potently HERG current (IHERG) recorded from HEK 293 cells stably expressing wild-type HERG (IC50 of ~16 nM).
References

[1]. https://www.ncbi.nlm.nih.gov/pubmed/15135665

 Chemical & Physical Properties

Density 1.161g/cm3
Boiling Point 632.6ºC at 760mmHg
Melting Point 158-162ºC
Molecular Formula C30H35F2N3O
Molecular Weight 491.61500
Flash Point 336.4ºC
Exact Mass 491.27500
PSA 35.58000
LogP 5.69880
Appearance of Characters white
Index of Refraction 1.581
Storage condition 2-8°C
Water Solubility DMSO: ≥10mg/mL

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TK7910000
CHEMICAL NAME :
1-Piperazineaceto-2',6'-xylidide, 4-(4,4-bis(p-fluorophenyl)butyl)-
CAS REGISTRY NUMBER :
3416-26-0
BEILSTEIN REFERENCE NO. :
0904339
LAST UPDATED :
199612
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C30-H35-F2-N3-O
MOLECULAR WEIGHT :
491.68

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
20570 ug/kg/8D-I
TOXIC EFFECTS :
Cardiac - arrhythmias (including changes in conduction)
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,923,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>3200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 32,461,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>3200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 32,461,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARPMAS Archiv der Pharmazie (Weinheim, Germany) (VCH Pub., Inc., 303 NW 12th Ave., Deerfield Beach, FL 33441) V.51-261, 1835-1923; V.305- 1972- Volume(issue)/page/year: 322,359,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
40 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2279383

 Safety Information

Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases R22
Safety Phrases 36
RIDADR NONH for all modes of transport
RTECS TK7910000

 Articles27

More Articles
Protective effects of the lazaroid U74500A and lidoflazine on liver preservation with UW solution.

Transpl. Int. 6(5) , 281-4, (1993)

The effect of adding a 21-aminosteroid, U74500A, and a Ca2+ antagonist, lidoflazine, alone and together to UW solution was assessed in a rat liver preservation model. Following preservation, the liver...

Simpson's paradox and clinical trials: what you find is not necessarily what you prove.

Ann. Emerg. Med. 21(12) , 1480-2, (1992)

Expensive clinical trials have become the gold standard for evaluating the efficacy of promising new therapeutic agents. Full exploration of the collected data is routine to maximize the yield of the ...

1,4-Dihydropyridines bearing a pharmacophoric fragment of lidoflazine.

Bioorg. Med. Chem. 4(10) , 1629-35, (1996)

A series of 1,4-dihydropyridines bearing a pharmacophoric fragment of lidoflazine was synthesized. The compounds were evaluated for inotropic, chronotropic, and calcium antagonist activities. All comp...

 Synonyms

4-[4,4-Bis(4-fluorophenyl)butyl]-N-(2,6-dimethylphenyl)-1-piperazineacetamide
2-[4-[4,4-bis(4-fluorophenyl)butyl]piperazin-1-yl]-N-(2,6-dimethylphenyl)acetamide
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  • Product Name: Lidoflazine
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
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