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Product Name: Enprofylline
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ShangHai DC Chemicals Co.,Ltd
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Dayang Chem (Hangzhou) Co., Ltd.
China
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Purity: 98.0%
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41078-02-8

41078-02-8 structure

Name: ENPROFYLLINE
Chemical Name: enprofylline
CAS Number: 41078-02-8
Molecular Formula: C₈H₁₀N₄O₂
Molecular Weight: 194.19100
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2018-06-17 16:18:42
Modify Date: 2024-01-08 05:28:19
Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].

Name	enprofylline
Synonyms	3,7-dihydro-3-propyl-1H-purine-2,6-dione enprophylline 3-propylxanthine Enprofilina [INN-Spanish] EINECS 255-201-8 3-propyl-7H-purine-2,6-dione Enprofilina Nilyph Oxeze Enprofyllinum [INN-Latin] Enprofyllinum 3-propylxanthine (PX) MFCD00043205 3-n-propylxanthine

Description	Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor
Target	A2B receptor:7 μM (Ki)
In Vitro	Enprofylline (300 μM) completely blocks the release of IL-8 by N-ethylcarboxamidoadenosine (NECA)[1]. Enprofylline (10 μM) inhibits NECA (10 μM) induced proliferation in a concentration-dependent manner[2]. Cell Proliferation Assay[2] Cell Line: Human retinal endothelial cells (HRECs) Concentration: 10 μM Incubation Time: 24, 48, 72 hours Result: NECA (10 μM) induced a time-dependent increase in HREC proliferation as measured by cell counts, achieving approximately 80% of the density of cells exposed to normal growth medium for 3 days. Enprofylline (10 μM) completely blocked the proliferative effect of NECA when added concurrently with the analogue.
In Vivo	Enprofylline increases heart rate (HR). Injection of Enprofylline (7.5 and 30 mg/kg) increases HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low and high dose, respectively[3]. A high dose of Enprofylline (30 mg/kg) also decreases temperature compared with saline injection in female (but not in males) WT mice, but a low dose (7.5 mg/kg) has little effect on mouse temperature[3]. Animal Model: A1RKO mice (were cross-bred to C57BL/6 mice for six generations) and A2ARKO mice (were backcrossed to C57BL/6 mice for more than 10 generations)[3] Dosage: 30 mg/kg Administration: Intraperitoneally injected (bolus) at 2-h intervals Result: Increased HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low (7.5 mg/kg) and high dose (30 mg/kg), respectively.
References	[1]. I Feoktistov, et al. Adenosine A2b receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. J Clin Invest. 1995 Oct;96(4):1979-86. [2]. M B Grant, et al. Proliferation, migration, and ERK activation in human retinal endothelial cells through A(2B) adenosine receptor stimulation. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2068-73. [3]. Jiang-Ning Yang, et al. Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. Am J Physiol Heart Circ Physiol. 2009 Apr;296(4):H1141-9.

Density	1.367 g/cm3
Molecular Formula	C₈H₁₀N₄O₂
Molecular Weight	194.19100
Exact Mass	194.08000
PSA	83.54000
Index of Refraction	1.583

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UO8439700

CHEMICAL NAME :: 1H-Purine-2,6-dione, 3,7-dihydro-3-propyl-

CAS REGISTRY NUMBER :: 41078-02-8

LAST UPDATED :: 199606

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C8-H10-N4-O2

MOLECULAR WEIGHT :: 194.22

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 :: 481 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLRCAT Pharmacological Research Communications. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1969- Volume(issue)/page/year: 22(Suppl 2),125,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 254 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLRCAT Pharmacological Research Communications. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1969- Volume(issue)/page/year: 22(Suppl 2),125,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 157 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex)

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 49,313,1981

Hazard Codes	Xn: Harmful;
Risk Phrases	R20/21/22
Safety Phrases	36
HS Code	2933990090

76194-09-7

~82%

41078-02-8

Literature: Sakai, Ryosuke; Konno, Kayo; Yamamoto, Yasunori; Sanae, Fujiko; Takagi, Kenzo; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4039 - 4044

14036-06-7

76194-07-5

~87%

41078-02-8

Literature: Cottam, Howard B.; Shih, Hsiencheng; Tehrani, Lida R.; Wasson, D. Bruce; Carson, Dennis A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 2 - 9

76194-07-5

~69%

41078-02-8

Literature: Aktiebolaget Draco Patent: US4325956 A1, 1982 ;

76194-05-3

41078-02-8

Literature: Cottam, Howard B.; Shih, Hsiencheng; Tehrani, Lida R.; Wasson, D. Bruce; Carson, Dennis A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 2 - 9

53681-47-3

41078-02-8

Literature: Cottam, Howard B.; Shih, Hsiencheng; Tehrani, Lida R.; Wasson, D. Bruce; Carson, Dennis A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 2 - 9

Precursor 4
14036-06-7 76194-07-5 76194-05-3 53681-47-3
DownStream 5
31542-62-8 31542-63-9 135462-21-4 121875-96-5
7464-76-8

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%

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