DC Chemicals Limited
China
Product Name: Epinastine HCl
Price: $300.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: EPINASTINE HYDROCHLORIDE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: EPINASTINE HYDROCHLORIDE
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

108929-04-0

108929-04-0 structure

Name: Epinastin HCl
Chemical Name: Epinastine Hydrochloride
CAS Number: 108929-04-0
Molecular Formula: C₁₆H₁₆ClN₃
Molecular Weight: 285.771
Catalog: API Antiallergic Antihistamine
Create Date: 2018-09-15 17:38:29
Modify Date: 2024-01-02 10:14:54
Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action[1][2][3].

Name	Epinastine Hydrochloride
Synonyms	9,13b-Dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-aminhydrochlorid UNII:GFM415S5XL 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azépin-3-amine chlorhydrate 9,13b-Dihydro-1H-dibenz[cf]imidazo[1,5-a]azepine hydrochloride,WAL-801Cl 1H-Dibenz[c,f]imidazo[1,5-a]azepin-3-amine, 9,13b-dihydro-, hydrochloride (1:1) 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride EPINASTINHCL Epinastine hydrochloride Epinastinehydrochloride 1H-Dibenz[c,f]imidazo[1,5-a]azepin-3-amine,9,13b-dihydro-,hydrochloride T B5 G6&6 BN DN CUT&T&J CZ &&HCl EPIMEDIUM P.E EPINASTINE HCL Epinastine 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine hydrochloride 1H-DIBENZ[C,F]IMIDAZO[1,5-A]AZEPIN-3-AMINE,9,13B-DIHYDRO-, HYDROCHLORIDE (1:1) 9,13b-Dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine hydrochloride (1:1) Epinastin HCl

Description	Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action[1][2][3].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Endocrinology Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
References	[1]. C Kamei, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205. [2]. T Roeder, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. ur J Pharmacol. 1998 May 22;349(2-3):171-7. [3]. T Kohyama, et al. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8.

Density	1.32g/cm3
Boiling Point	428ºC at 760 mmHg
Melting Point	>270ºC
Molecular Formula	C₁₆H₁₆ClN₃
Molecular Weight	285.771
Flash Point	212.7ºC
Exact Mass	285.103271
PSA	41.62000
LogP	3.46970
Vapour Pressure	1.56E-07mmHg at 25°C
Storage condition	2-8°C
Water Solubility	H2O: soluble38mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO4360000

CHEMICAL NAME :: IH-Dibenz(c,f)imidazo(1,5-a)azepin-3-amine, 9,13b-dihydro-, hydrochloride

CAS REGISTRY NUMBER :: 108929-04-0

LAST UPDATED :: 199210

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H15-N3.Cl-H

MOLECULAR WEIGHT :: 285.80

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 :: 192 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Gastrointestinal - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 13650 mg/kg/13W-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in endocrine weight (unspecified) Blood - changes in platelet count

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 36400 mg/kg/52W-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Endocrine - changes in endocrine weight (unspecified) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 13 gm/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8400 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 975 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301
Precautionary Statements	P301 + P310
Personal Protective Equipment	Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes	T: Toxic;
Risk Phrases	R25
Safety Phrases	45
RIDADR	UN 2811 6
RTECS	HO4360000
HS Code	2933990090

80012-43-7

~90%

108929-04-0

Literature: USV LIMITED Patent: WO2009/63504 A2, 2009 ; Location in patent: Page/Page column 25 ;

4998-12-3

108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

80012-69-7

108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

41218-84-2

108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

127786-29-2

108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

Precursor 4
80012-43-7 80012-69-7 41218-84-2 127786-29-2
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

108929-04-0	80012-44-8
127786-29-2	1700663-41-7
2711717-77-8	16154-78-2
1115177-19-9	864374-00-5
82640-04-8	1049788-58-0