α-Fluoromethylhistidine dihydrochloride

Name: α-Fluoromethylhistidine dihydrochloride
Brand: MedChemExpress
SKU: HY-115822
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Cat. No.: HY-115822 Pureza: 99.1%: Ficha de datos
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α-Fluoromethylhistidine dihydrochloride is an orally active histidine decarboxylase inhibitor. α-Fluoromethylhistidine dihydrochloride depletes histamine in enterochromaffin-like (ECL) cells, reduces the number and volume density of secretory vesicles in ECL cells, and does not affect histamine storage in mast cells. α-Fluoromethylhistidine dihydrochloride abolishes Omeprazole (HY-B0113)-induced vacuolization of ECL cells and decreases gastrin-induced histamine efflux from ECL cells. α-Fluoromethylhistidine dihydrochloride does not alter the granular characteristics of ECL cells, omeprazole-induced hypertrophy of ECL cells, gastrin-induced pancreastatin-like immunoreactivity efflux, nor does it affect gastric acid secretion induced by histamine or vagal stimulation. α-Fluoromethylhistidine dihydrochloride inhibits basal and gastrin-stimulated gastric acid secretion, reduces acid output induced by gastrin+IBMX (HY-12318), but does not directly affect acid generation in isolated parietal cells.

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α-Fluoromethylhistidine dihydrochloride Estructura química

No. CAS : 81839-27-2

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1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
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Other Forms of α-Fluoromethylhistidine dihydrochloride:

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In Vivo

α-Fluoromethylhistidine (dihydrochloride) (3 mg/kg per h; subcutaneous; continuous infusion; 6 weeks) depletes ECL cell histamine, reduces ECL cell secretory vesicle and microvesicle numbers, and alters secretory vesicle size, but does not affect ECL cell hypertrophy or granule ultrastructure in female Sprague-Dawley rats^[1].
α-Fluoromethylhistidine (dihydrochloride) (3 mg/kg per h; subcutaneous; continuous infusion; 6 weeks) depletes ECL cell histamine, abolishes omeprazole-induced ECL cell vacuole formation, reduces ECL cell secretory vesicle and microvesicle numbers and volume density, but does not affect omeprazole-induced ECL cell hypertrophy or granule ultrastructure in female Sprague-Dawley rats with omeprazole-induced hypergastrinemia^[1].
α-Fluoromethylhistidine (dihydrochloride) (3 mg/kg per h; subcutaneous; 24 h) reduces mouse oxyntic mucosal histamine by ~65%, depletes ECL cell secretory vesicles by ~84%, and increases plasma gastrin levels by 130%^[2].
α-Fluoromethylhistidine (dihydrochloride) (3 mg/kg per h; subcutaneous; 24 h) reduces rat oxyntic mucosal histamine by ~83%, depletes ECL cell secretory vesicles by ~88%, increases plasma gastrin levels by 143%, and does not affect other gastric oxyntic endocrine cell types^[2].
α-Fluoromethylhistidine (dihydrochloride) (3 mg/kg per h; subcutaneous; 24 h) reduces hamster oxyntic mucosal histamine by ~91%, depletes ECL cell secretory vesicles by ~89%, and reduces ECL cell profile size by ~33%, with no effect on plasma gastrin levels^[2].
α-Fluoromethylhistidine (dihydrochloride) (5 mg/kg/h; s.c.; continuous; 24 hours) produces 80% depletion of oxyntic mucosal histamine via irreversible inhibition of HDC, while leaving oxyntic mucosal pancreastatin-LI concentrations unaltered in male Sprague-Dawley rats^[3].
α-Fluoromethylhistidine (3 mg/kg/h, 50 mg/kg; s.c., p.o.; continuous infusion, single dose; 2-6 days, 2 hours before testing) reduces oxyntic mucosal histamine by 80%, inhibits basal gastric acid secretion by over 60%, and almost abolishes gastrin-17-stimulated acid secretion, but does not alter histamine-stimulated or vagally induced (insulin or pylorus ligation) gastric acid secretion in female Sprague-Dawley rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sprague-Dawley (female, 200-225 g)^[1]
Dosage:	3 mg/kg per h
Administration:	subcutaneous; continuous infusion; 6 weeks
Result:	Left ECL cell profile area, cytoplasm area, and nucleus area unchanged relative to control rats. Left ECL cell granule number per cell profile (7.0), granule volume density (1.6% cytoplasm), and granule median diameter (115-125 nm) unchanged relative to control rats. Reduced ECL cell secretory vesicle number per cell profile (19.7) and volume density (7.7% cytoplasm) significantly relative to control rats (P<0.01); remaining secretory vesicles had a smaller median diameter (165 nm vs. 180 nm in controls). Reduced ECL cell microvesicle number per cell profile (11.0) significantly relative to control rats (P<0.05), while left microvesicle volume density (3.4% cytoplasm) unchanged. Showed no vacuoles in ECL cells of treated rats. Caused granules and secretory vesicles in treated rats to have large, diffuse, weakly electron-dense cores.

Animal Model:	Sprague-Dawley rats (female, 250-280 g body weight)^[2]
Dosage:	3 mg/kg per h
Administration:	subcutaneous; continuous; 24 h
Result:	Reduced oxyntic mucosal histamine concentration from 36.7 µg/g wet weight (control) to 6.2 µg/g wet weight (P<0.001). Lost histamine immunostaining from ECL cells but retained it in mast cells. Reduced number of ECL cell secretory vesicles per cell profile from 42 (control) to 5 (P<0.01). Reduced volume density of ECL cell secretory vesicles (as a % of cytoplasm) from 16 (control) to 1 (P<0.01). Caused no significant changes in ECL cell profile area, cytoplasm profile area, nuclear profile area, nuclear volume density, granule number or volume density, or microvesicle number or volume density. Increased plasma gastrin concentration from 140 pg/mL (control) to 340 pg/mL (P<0.001). Caused no changes in the ultrastructure or morphometric parameters of rat A-like cells, somatostatin cells, or D₁/P cells.

Peso molecular

260.09

Fòrmula

C₇H₁₂Cl₂FN₃O₂

No. CAS

81839-27-2

Appearance

Solid

Color

White to off-white

SMILES

N[C@](CC1=CNC=N1)(CF)C(O)=O.Cl.Cl

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Pureza y Documentación

Purity: 99.1%

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Referencias

[1]. Chen D, et al. Ultrastructure of enterochromaffin-like cells in rat stomach: effects of alpha-fluoromethylhistidine-evoked histamine depletion and hypergastrinemia. Cell Tissue Res. 1996;283(3):469-478. [Content Brief]

[2]. Andersson K, et al. Effect of alpha-fluoromethylhistidine-evoked histamine depletion on ultrastructure of endocrine cells in acid-producing mucosa of stomach in mouse, rat and hamster. Cell Tissue Res. 1996;286(3):375-384.

[3]. Chen D, et al. Gastrin-evoked secretion of pancreastatin and histamine from ECL cells and of acid from parietal cells in isolated, vascularly perfused rat stomach. Effects of isobutyl methylxanthin and alpha-fluoromethylhistidine. Regul Pept. 1996;65(2):133-138.

[4]. Andersson K, et al. Gastric acid secretion after depletion of enterochromaffin-like cell histamine. A study with alpha-fluoromethylhistidine in rats. Scand J Gastroenterol. 1996;31(1):24-30.