Introduction：Basic information about CAS 41078-02-8|ENPROFYLLINE, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | ENPROFYLLINE |
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| CAS Number | 41078-02-8 | Molecular Weight | 194.19100 |
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| Density | 1.367 g/cm3 | Boiling Point | / |
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| Molecular Formula | C8H10N4O2 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | enprofylline |
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| Synonym | More Synonyms |
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ENPROFYLLINE BiologicalActivity
| 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]. |
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| Related Catalog | Signaling Pathways >>Metabolic Enzyme/Protease >>Phosphodiesterase (PDE)Research Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Adenosine Receptor |
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| Target | A2B receptor:7 μM (Ki) |
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| 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. |
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| 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. |
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| 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. |
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Chemical & Physical Properties
| Density | 1.367 g/cm3 |
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| Molecular Formula | C8H10N4O2 |
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| Molecular Weight | 194.19100 |
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| Exact Mass | 194.08000 |
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| PSA | 83.54000 |
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| Index of Refraction | 1.583 |
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| InChIKey | SIQPXVQCUCHWDI-UHFFFAOYSA-N |
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| SMILES | CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 |
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Toxicological Information
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 DATAACUTE 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
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Safety Information
| Hazard Codes | Xn: Harmful; |
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| Risk Phrases | R20/21/22 |
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| Safety Phrases | 36 |
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| HS Code | 2933990090 |
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Customs
| HS Code | 2933990090 |
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| 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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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 |
