EFAROXAN HYDROCHLORIDE

Product Name: EFAROXAN HYDROCHLORIDE
CAS No.: 89197-00-2
Chemical Name: EFAROXAN HYDROCHLORIDE
Synonyms: RX 821037A;EfaroxanHCl;Zinc00002748;PO20090827-Efaroxan;EFAROXAN HYDROCHLORIDE;(+/-)-efaroxan hydrochloride;Efaroxan hydrochloride >=98% (HPLC);2-ETHYL-2-(IMIDAZOLIN-2-YL)-2,3-DIHYDROBENZOFURAN HYDROCHLORIDE;2-(2-ETHYL-2,3-DIHYDROBENZOFURAN-2-YL)-4,5-DIHYDRO-1H-IMIDAZOLE HCL;2-(2-ETHYL-2,3-DIHYDRO-2-BENZOFURANYL)-4,5-DIHYDRO-1H-IMIDAZOLE HYDROCHLORIDE
CBNumber: CB9376896
Molecular Formula: C13H17ClN2O
Formula Weight: 252.74
MOL File: 89197-00-2.mol

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EFAROXAN HYDROCHLORIDE Property

storage temp.: Store at RT
solubility: H₂O: 300 mg/mL
form: solid
color: White
Water Solubility: Soluble to 100 mM in water
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 1 month.
InChI: InChI=1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13;/h3-6H,2,7-9H2,1H3,(H,14,15);1H
InChIKey: DWOIUCRHVWIHAH-UHFFFAOYSA-N
SMILES: C(C1(C2NCCN=2)OC2C=CC=CC=2C1)C.Cl

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Safety

Hazard Codes: T
Risk Statements: 25
Safety Statements: 7-35-45
RIDADR: UN 2811 6.1/PG 3
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger
Hazard statements: H301Toxic if swalloed
Precautionary statements: P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: E3263
Product name: Efaroxan hydrochloride
Purity: ≥98% (HPLC)
Packaging: 10mg
Price: $77.7
Updated: 2025/07/31

Sigma-Aldrich

Product number: E3263
Product name: Efaroxan hydrochloride
Purity: ≥98% (HPLC)
Packaging: 50mg
Price: $322
Updated: 2025/07/31

Cayman Chemical

Product number: 29008
Product name: Efaroxan (hydrochloride)
Packaging: 25mg
Price: $72
Updated: 2024/03/01

Cayman Chemical

Product number: 29008
Product name: Efaroxan (hydrochloride)
Packaging: 50mg
Price: $98
Updated: 2024/03/01

Cayman Chemical

Product number: 29008
Product name: Efaroxan (hydrochloride)
Packaging: 10mg
Price: $37
Updated: 2024/03/01

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EFAROXAN HYDROCHLORIDE Chemical Properties,Usage,Production

Description

Efaroxan HCl (89197-00-2) is a selective α2-adrenergic receptor antagonist1 (selectivity ratio of α2/α1 = 724)4 and imidazoline receptor antagonist2. Induces release of insulin in the rat insulinoma cell line RIN-5AH by interaction with ATP-sensitive potassium channels independently from imidazoline I1 or I2 receptors.3 Efaroxan HCl increases resting plasma insulin levels and markedly potentiates the rise in insulin levels produced by adrenaline in the rat.4

Uses

Efaroxan Hydrochloride is a potent α2-AR adrenoceptor antagonist.

Biological Activity

Potent, highly selective α 2 adrenoceptor antagonist and imidazoline I 1 receptor ligand (pK i values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A , α 2B , α 2C , I 1 , and I 2 receptors respectively). Promotes insulin secretion, at a site distinct from I 1 or I 2 (the putative I 3 receptor) in vitro and in vivo .

in vivo

Efaroxan hydrochloride increases plasma insulin levels in both conscious fed and fasted rats without greatly affecting plasma glucoselevels^[3].

Animal Model:	Male Sprague-Dawley rats (weight range 250-300g)^[3]
Dosage:	1 mg/kg, 5 mg/kg
Administration:	Oral administration
Result:	Produced a significant increase in plasma insulin levels of starved rats 15 and 30 min after treatment.

IC 50

α adrenergic receptor

References

[1] CHRISTOPHER B. CHAPLEO. .alpha.-Adrenoceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on .alpha.-adrenoreceptor activity[J]. Journal of Medicinal Chemistry, 1984, 27 5: 570-576. DOI:10.1021/jm00371a003
[2] R M EGLEN. “Seeing through a glass darkly”: casting light on imidazoline “I” sites.[J]. Trends in pharmacological sciences, 1998, 19 9: 381-390. DOI:10.1016/s0165-6147(98)01244-9
[3] GABRIEL OLMOS . Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors[J]. European journal of pharmacology, 1994, 262 1: Pages 41-48. DOI:10.1016/0014-2999(94)90026-4
[4] TIMOTHY L. BERRIDGE Alan G R John C Doxey. Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats[J]. European journal of pharmacology, 1992, 213 2: Pages 213-218. DOI:10.1016/0014-2999(92)90684-v

EFAROXAN HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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EFAROXAN HYDROCHLORIDE Suppliers

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89197-00-2, EFAROXAN HYDROCHLORIDERelated Search:

Butyramidine hydrochloride 2-PHENOXYACETAMIDINE HYDROCHLORIDE 2-METHOXYACETAMIDINE HYDROCHLORIDE 2-Methyl-1-phenyl-2-propanol BUTYRAMIDINE 1-(2,3-DIHYDRO-1-BENZOFURAN-2-YL)METHANAMINE HYDROCHLORIDE Efaroxan 2-BENZYL-2-BUTANOL propionamidine hydrochloride 2-METHOXY-2-METHYL-PROPYLAMINE 2-METHYLPROPANIMIDAMIDE HYDROCHLORIDE 2-PHENOXYPROPYLAMINE HYDROCHLORIDE IMIDAZOLE HYDROCHLORIDE 2,3-Dihydrobenzofuran EFAROXAN HYDROCHLORIDE 1-(AMINOMETHYL)-CYCLOPROPANOL 2-(2-methylphenoxy)ethanamine 2-HYDROXY-PROPIONAMIDINE

EFAROXAN HYDROCHLORIDE

2-ETHYL-2-(IMIDAZOLIN-2-YL)-2,3-DIHYDROBENZOFURAN HYDROCHLORIDE

(+/-)-2-(2-ETHYL-2,3-DIHYDRO-2-BENZOFURANYL)-4,5-DIHYDRO-1H-IMIDAZOLE HYDROCHLORIDE

2-(2-Ethyl-2,3-dihydrobenzofuran-2-yl)-4,5-dihydro-1H-imidazole hydrochloride

EfaroxanHCl

RX 821037A, 2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran hydrochloride

Zinc00002748

RX 821037A

1H-Imidazole,2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-,monohydrochloride

2-(2-ETHYL-2,3-DIHYDROBENZOFURAN-2-YL)-4,5-DIHYDRO-1H-IMIDAZOLE HCL

2-(2-ETHYL-2,3-DIHYDRO-2-BENZOFURANYL)-4,5-DIHYDRO-1H-IMIDAZOLE HYDROCHLORIDE

PO20090827-Efaroxan

(+/-)-efaroxan hydrochloride

Efaroxan hydrochloride >=98% (HPLC)

89197-00-2

88917-00-2

Adrenoceptor