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Postion:Product Catalog >Analytical Chemistry>Standard>Pharmaceutical Impurity Reference Standards> cephaeline hydrochloride
	cephaeline hydrochloride
  • 	cephaeline hydrochloride
  • 	cephaeline hydrochloride

cephaeline hydrochloride NEW

Price $8 $6 $1
Package 1kg 25kg 100kg
Min. Order: 1kg
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-29

Product Details

Product Name: cephaeline hydrochloride CAS No.: 5853-29-2
Min. Order: 1kg Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/29
Lead time: In stock, ready for shipment Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
COA, MSDS: Available, contact us for details Name: Sun

 1. Materials information

Names

Name(-)-cephaeline dihydrochloride
SynonymMore Synonyms

 Cephaeline Dihydrochloride Biological Activity

Description(-)-Cephaeline dihydrochloride is an enantiomer of Cephaeline dihydrochloride. Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with IC50 of 121 μM.
Related Catalog
Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450
Research Areas >> Others
Target

IC50: 121 μM (CYP2D6)[1] Ki: 54 μM (CYP2D6)[1]

In VitroCYP2D6 reveals the highest metabolic activity for the generation of 9-O-demethylEmetine, whereas this enzyme also shows a significant metabolic activity for the generation of Cephaeline. IC50 of Cephaeline against CYP2C9, CYP2D6 and CYP3A4 is over 1000, 121 and 1000 μM, respectively. Further experiments are performed to determine inhibition constants (Ki) for Cephaeline on the CYP2D6 and CYP3A4 activities Graphic analysis of Dixon plots at various Cephaeline concentrations for each of the two CYP enzyme assays yield Kis of 54 and 355 μM for CYP2D6 and CYP3A4, respectively[1].
Kinase AssayCephaeline is dissolved in methanol to give concentrations of 0.1, 1, 10, 100 μM (only theophylline-O-demethylase activity with Cephaeline; 0.0985, June 2001 679 0.985, 9.85, 98.5 μM) [1]. Human liver microsomal protein is incubated with the selected marker substrates in the absence and presence of above concentrations of Cephaeline or Emetine (1-100 μM, only theophylline-O-demethylase activity with Cephaeline; 0.0985—98.5 μM, final concentration). Incubation conditions are chosen such that the product formation is linear with respect to both incubation times and protein concentrations, with substrate concentrations being at or below the Km for each enzyme. The effects of furafylline, sulphaphenazole, tranylcypromine, quinidine, and ketoconazole, selective inhibitors of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, respectively, are also determined in the same microsomal samples to provide comparisons with inhibitory potentials (IC50) of Cephaeline and Emetine towards the individual CYP form. The Ki s for Cephaeline and Emetine are determined by using the same pooled microsomal sample. This is achieved by varying the initial substrate concentrations (bufuralol 8, 16 and 32 μM; testosterone 45, 90 and 180u M) and using several inhibitor concentrations of 10, 50, and 100 μM. The Kis are estimated by graphic analysis of Dixon plots. These values are subsequently used as initial estimates for the nonlinear least-squares regression analysis[1].
References

[1]. Asano T, et al. Metabolism of ipecac alkaloids Cephaeline and Emetine by human hepatic microsomal cytochrome P450s, and their inhibitory effects on P450 enzyme activities. Biol Pharm Bull. 2001 Jun;24(6):678-82.

 Chemical & Physical Properties

Molecular FormulaC28H40Cl2N2O4
Molecular Weight539.53
PSA63.19000
LogP5.70910

 Toxicological Information

CHEMICAL IDENTIFICATION

  • RTECS NUMBER :

  • FJ9450000

  • CHEMICAL NAME :

  • Cephaeline hydrochloride

  • CAS REGISTRY NUMBER :

  • 5853-29-2

  • LAST UPDATED :

  • 199206

  • DATA ITEMS CITED :

  • 5

  • MOLECULAR FORMULA :

  • C28-H38-N2-O4.2Cl-H

  • MOLECULAR WEIGHT :

  • 539.60

  • WISWESSER LINE NOTATION :

  • T B666 GNTT&J E2 LO1 MO1 D1- BT66 CMT&J HQ IO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Intraperitoneal

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 10 mg/kg

  • TOXIC EFFECTS :

  • Details of toxic effects not reported other than lethal dose value

  • REFERENCE :

  • JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 104,421,1952

  • TYPE OF TEST :

  • LDLo - Lowest published lethal dose

  • ROUTE OF EXPOSURE :

  • Subcutaneous

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 6500 ug/kg

  • TOXIC EFFECTS :

  • Details of toxic effects not reported other than lethal dose value

  • REFERENCE :

  • JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 10,73,1917/1918

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - mouse

  • DOSE/DURATION :

  • 74970 ug/kg

  • TOXIC EFFECTS :

  • Details of toxic effects not reported other than lethal dose value

  • REFERENCE :

  • NCISP* National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program. (Bethesda, MD 20205) Volume(issue)/page/year: JAN1986

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Intraperitoneal

  • SPECIES OBSERVED :

  • Rodent - mouse

  • DOSE/DURATION :

  • 20530 ug/kg

  • TOXIC EFFECTS :

  • Details of toxic effects not reported other than lethal dose value

  • REFERENCE :

  • NCISP* National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program. (Bethesda, MD 20205) Volume(issue)/page/year: JAN1986

  • TYPE OF TEST :

  • LDLo - Lowest published lethal dose

  • ROUTE OF EXPOSURE :

  • Subcutaneous

  • SPECIES OBSERVED :

  • Rodent - guinea pig

  • DOSE/DURATION :

  • 8 mg/kg

  • TOXIC EFFECTS :

  • Details of toxic effects not reported other than lethal dose value

  • REFERENCE :

  • JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 10,73,1917/1918

 Safety Information

RIDADR1544
Packaging GroupIII
Hazard Class6.1(b)

 Synonyms

10,11,7'-Trimethoxy-emetan-6'-ol,Hydrochlorid
cephaeline dihydrochloride
10,11,7'-trimethoxy-emet-1'-ene-9,6'-diol
Alangicine
10,11,7'-trimethoxy-emetan-6'-ol,dihydrochloride
10,11,7'-Trimethoxy-emetan-6'-ol,Dihydrochlorid
EINECS 227-463-3
(-)-Cephaeline (dihydrochloride)

Equipoise
10-Undecenoic acid, (17β)-3-oxoandrosta-1,4-dien-17-yl ester
Androsta-1,4-dien-3-one, 17-[(1-oxo-10-undecenyl)oxy]-, (17β)-
Boldenone 10-undecenoate
Boldenone Undecylenate
boldenone undec-10-enoate
Androsta-1,4-dien-3-one, 17-β-hydroxy-, 10-undecenoate
17b-[(1-Oxo-10-undecenyl)oxy]-androsta-1,4-dien-3-one
[(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] undec-10-enoate
MFCD00079126
(17β)-3-Oxoandrosta-1,4-dien-17-yl 10-undecenoate
17β-Hydroxyandrosta-1,4-dien-3-one 10-undecenoate





2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


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3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

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4. Contact information

For more details, pls contact us freely.

Email address: Sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137











Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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