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  • Product Name: Lidoflazine
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3416-26-0

3416-26-0 structure
3416-26-0 structure
  • Name: Lidoflazine
  • Chemical Name: Lidoflazine
  • CAS Number: 3416-26-0
  • Molecular Formula: C30H35F2N3O
  • Molecular Weight: 491.61500
  • Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
  • Create Date: 2018-10-04 05:47:25
  • Modify Date: 2024-01-11 19:58:42
  • 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].

Name Lidoflazine
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
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

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 white
Index of Refraction 1.581
Storage condition 2-8°C
Water Solubility DMSO: ≥10mg/mL

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
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