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119615-63-3

119615-63-3 structure
119615-63-3 structure
  • Name: Olprinone (Hydrochloride)
  • Chemical Name: 5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-1H-pyridine-3-carbonitrile,hydrochloride
  • CAS Number: 119615-63-3
  • Molecular Formula: C14H11ClN4O
  • Molecular Weight: 286.72
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
  • Create Date: 2019-01-13 11:31:29
  • Modify Date: 2024-01-07 16:06:30
  • Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
Name 5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-1H-pyridine-3-carbonitrile,hydrochloride
Synonyms E 1020
pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile hydrochloride
Olprinone hydrochloride
Olprinone (Hydrochloride)
1,2-dihydro-5-imidazo<1,2-a>pyridin-6-yl-6-methyl-2-oxo-3-pyridine carbonitrile hydrochloride
1,2-dihydro-6-methyl-2-oxo-5-(imidazo[1,2-a]pyridin-6-yl)-3-pyridine carbonitrile hydrochloride
MFCD01749474
Loprinone hydrochloride
Description Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
Related Catalog
References

[1]. Tsubokawa T, Ishizuka S, Fukumoto K, et al. The effect of hemodilution by cardiopulmonary bypass on protein binding of olprinone. J Anesth. 2012 .

[2]. Mokra D, Drgova A, Pullmann R Sr, et al. Selective phosphodiesterase 3 inhibitor olprinone attenuates meconium-induced oxidative lung injury. Pulm Pharmacol Ther. 2012 Jun;25(3):216-22.

[3]. Yamanaka H, Hayashi Y, Kamibayashi T, Mashimo T. Effect of olprinone, a phosphodiesterase III inhibitor, on balance of cerebral oxygen supply and demand during cardiopulmonary bypass. J Cardiovasc Pharmacol. 2011 May;57(5):579-83.

[4]. Mazzon E, Esposito E, Di Paola R, et al. Olprinone, a specific phosphodiesterase (PDE)-III inhibitor, reduces the development of multiple organ dysfunction syndrome in mice. Pharmacol Res. 2011 Jul;64(1):68-79.
Density 1.34g/cm3
Melting Point >300ºC
Molecular Formula C14H11ClN4O
Molecular Weight 286.72
PSA 83.18000
LogP 2.60738
Storage condition 2-8℃

CHEMICAL IDENTIFICATION

RTECS NUMBER :
US4201450
CHEMICAL NAME :
3-Pyridinecarbonitrile, 1,2-dihydro-5-(imidazo(1,2-a)pyridin-6-yl)-6-methyl-2 -oxo-, monohydrochloride, monohydrate
CAS REGISTRY NUMBER :
119615-63-3
LAST UPDATED :
199703
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C14-H10-N4-O.Cl-H.H2-O
MOLECULAR WEIGHT :
304.76

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 :
7804 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2133 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
176 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - tremor
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3898 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
242 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>100 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Gastrointestinal - nausea or vomiting
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
175 mg/kg/4W-I
TOXIC EFFECTS :
Behavioral - fluid intake Cardiac - EKG changes not diagnostic of specified effects Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
11 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
130 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Micronucleus test

MUTATION DATA

TYPE OF TEST :
Cytogenetic analysis
TEST SYSTEM :
Rodent - hamster Lung
DOSE/DURATION :
1200 mg/L
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,77,1993
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases S26
RIDADR NONH for all modes of transport
RTECS US4201450

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