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Postion:Product Catalog >Analytical Chemistry>Standard>Pharmaceutical Impurity Reference Standards>EMEDASTINE FUMARATE
EMEDASTINE FUMARATE
  • EMEDASTINE FUMARATE
  • EMEDASTINE FUMARATE

EMEDASTINE FUMARATE NEW

Price $32 $1.3
Package 1KG 1000KG
Min. Order: 1KG
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-04-15

Product Details

Product Name: EMEDASTINE FUMARATE CAS No.: 87233-62-3
Min. Order: 1KG Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/04/15
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: Mia

1. Materials information

Names

Nameemedastine difumarate
SynonymMore Synonyms

 emedastine fumarate Biological Activity

DescriptionEmedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
Related Catalog
Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Target

H1 Receptor:1.3 nM (Ki)

H2 Receptor:49067 nM (Ki)

H3 Receptor:12430 nM (Ki)

In VitroEmedastine difumarate inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1]. High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2]. Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].
In VivoEmedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3]. Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3]. Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2]. Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2]. Animal Model: Male ICR mice 5-6 weeks of age[3] Dosage: 0.03, 0.1, 0.3 mg/kg Administration: Orally; 30 min before pruritogen injection Result: Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
References

[1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64.

[2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.

[3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.

 Chemical & Physical Properties

Boiling Point446.6oC at 760 mmHg
Melting Point148-151°
Molecular FormulaC25H34N4O9
Molecular Weight534.55900
Exact Mass534.23300
PSA182.73000
LogP1.64120
Storage condition2-8°C
Water SolubilitySoluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.

 MSDS

emedastine fumarate MSDS(Chinese)

 Toxicological Information

CHEMICAL IDENTIFICATION

  • RTECS NUMBER :

  • DD8870000

  • CAS REGISTRY NUMBER :

  • 87233-62-3

  • LAST UPDATED :

  • 199503

  • DATA ITEMS CITED :

  • 12

  • MOLECULAR FORMULA :

  • C17-H26-N4-O.2C4-H4-O4

  • MOLECULAR WEIGHT :

  • 534.63

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 1854 mg/kg

  • TOXIC EFFECTS :

  • Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Subcutaneous

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 643 mg/kg

  • TOXIC EFFECTS :

  • Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Intravenous

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 72 mg/kg

  • TOXIC EFFECTS :

  • Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - mouse

  • DOSE/DURATION :

  • 2206 mg/kg

  • TOXIC EFFECTS :

  • Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Subcutaneous

  • SPECIES OBSERVED :

  • Rodent - mouse

  • DOSE/DURATION :

  • 609 mg/kg

  • TOXIC EFFECTS :

  • Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Intravenous

  • SPECIES OBSERVED :

  • Rodent - mouse

  • DOSE/DURATION :

  • 93 mg/kg

  • TOXIC EFFECTS :

  • Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Mammal - dog

  • DOSE/DURATION :

  • 193 mg/kg

  • TOXIC EFFECTS :

  • Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate increase, without fall in BP

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

  • TYPE OF TEST :

  • LD50 - Lethal dose, 50 percent kill

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - guinea pig

  • DOSE/DURATION :

  • 744 mg/kg

  • TOXIC EFFECTS :

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

  • REFERENCE :

  • ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 34,801,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA **

  • TYPE OF TEST :

  • TDLo - Lowest published toxic dose

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 22750 mg/kg/13W-I

  • TOXIC EFFECTS :

  • Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,215,1990

  • TYPE OF TEST :

  • TDLo - Lowest published toxic dose

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Rodent - rat

  • DOSE/DURATION :

  • 18250 mg/kg/1Y-I

  • TOXIC EFFECTS :

  • Liver - other changes Endocrine - changes in pituitary weight Related to Chronic Data - changes in prostate weight

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,269,1990

  • TYPE OF TEST :

  • TDLo - Lowest published toxic dose

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Mammal - dog

  • DOSE/DURATION :

  • 6825 mg/kg/13W-I

  • TOXIC EFFECTS :

  • Behavioral - convulsions or effect on seizure threshold Blood - changes in spleen Related to Chronic Data - death

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,231,1990

  • TYPE OF TEST :

  • TDLo - Lowest published toxic dose

  • ROUTE OF EXPOSURE :

  • Oral

  • SPECIES OBSERVED :

  • Mammal - dog

  • DOSE/DURATION :

  • 16425 mg/kg/1Y-I

  • TOXIC EFFECTS :

  • Liver - changes in liver weight Related to Chronic Data - changes in prostate weight Related to Chronic Data - changes in testicular weight

  • REFERENCE :

  • OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,285,1990

 Safety Information

RIDADRNONH for all modes of transport
RTECSDD8870000
HS Code2933990090

 Customs

HS Code2933990090
Summary2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%


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: mia@fdachem.com

Mob: 86 18336764634

WhatsApp/Skype/Wechat/LINE: 86 18336764634










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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