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72956-09-3

72956-09-3 structure
72956-09-3 structure
  • Name: Carvedilol
  • Chemical Name: carvedilol
  • CAS Number: 72956-09-3
  • Molecular Formula: C24H26N2O4
  • Molecular Weight: 406.474
  • Catalog: API Circulatory system medication Peripheral vasodilator
  • Create Date: 2018-02-07 08:00:00
  • Modify Date: 2024-01-02 18:46:46
  • Carvedilol(BM14190) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.IC50 Value: 3.8 μM ( inhibition of LDL oxidation)Target: beta Adrenergic ReceptorCarvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.
Name carvedilol
Synonyms (±)-1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
Coropress
1-(9H-Carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}-2-propanol
Dilatrend
Carvedilolum
1-(9H-carbazol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol
Kredex
1-(9H-carbazol-4-yloxy)-3-{[2-(2-méthoxyphénoxy)éthyl]amino}propan-2-ol
2-propanol, 1-(9H-carbazol-4-yloxy)-3-2-(2-methoxyphenoxy)ethylamino-
Coreg
1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol
1-(9H-carbazol-4-yloxy)-3-[(2-{[2-(methyloxy)phenyl]oxy}ethyl)amino]propan-2-ol
Dimitone
2-Propanol, 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-
Carvedilolum [Latin]
MFCD00864692
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
1-[carbazolyl-(4)-oxy]-3-[(2-methoxyphenoxyethyl)amino]-propanol-(2)
Querto
1-(9H-carbazol-4-yloxy)-3-{2-(2-methoxyphenoxy)ethylamino}propan-2-ol
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxy-phenoxy)-ethylamino]-propan-2-ol
Carvedilol
Eucardic
Description Carvedilol(BM14190) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.IC50 Value: 3.8 μM ( inhibition of LDL oxidation)Target: beta Adrenergic ReceptorCarvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.
Related Catalog
References

[1]. Chen J, Huang C, Zhang B, et al. The effects of carvedilol on cardiac structural remodeling: The role of endogenous nitric oxide in the activity of carvedilol. Mol Med Rep. 2013 Apr;7(4):1155-8.

[2]. Stafylas PC, Sarafidis PA. Carvedilol in hypertension treatment. Vasc Health Risk Manag. 2008;4(1):23-30.

[3]. Othman AA, Tenero DM, Boyle DA et al. Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate. AAPS J. 2007 Jun 15;9(2):E208-1

[4]. Koshimizu TA, Tsujimoto G, Hirasawa A et al. Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-72.
Density 1.3±0.1 g/cm3
Boiling Point 655.2±55.0 °C at 760 mmHg
Melting Point 113-117ºC
Molecular Formula C24H26N2O4
Molecular Weight 406.474
Flash Point 350.1±31.5 °C
Exact Mass 406.189270
PSA 75.74000
LogP 4.11
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.657
Storage condition Store at +4°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UA8670000
CHEMICAL NAME :
2-Propanol, 1-(9H-carbazol-4-yloxy)-3-((2-(2-methoxyphenoxy)ethyl )amino)-
CAS REGISTRY NUMBER :
72956-09-3
LAST UPDATED :
199612
DATA ITEMS CITED :
14
MOLECULAR FORMULA :
C24-H26-N2-O4
MOLECULAR WEIGHT :
406.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
8 gm/kg
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,1181,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
769 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - acute pulmonary edema
REFERENCE :
NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
25 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Liver - other changes
REFERENCE :
NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
8 gm/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,1181,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
364 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - acute pulmonary edema
REFERENCE :
NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
27 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Olfaction) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Liver - other changes
REFERENCE :
NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,135,1987
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,1181,1989 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3 gm/kg
SEX/DURATION :
female 7-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 25,3101,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1620 mg/kg
SEX/DURATION :
female 16-21 day(s) after conception lactating female 1-21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
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: 25,3109,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
36 gm/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
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: 25,3071,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
36 gm/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - live birth index (measured after birth)
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: 25,3071,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
36 gm/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical
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: 25,3071,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1950 mg/kg
SEX/DURATION :
female 7-19 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)
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: 25,127,1991
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
975 mg/kg
SEX/DURATION :
female 7-19 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord)
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: 25,127,1991
Symbol GHS09
GHS09
Hazard Statements H411
Precautionary Statements P273
Personal Protective Equipment Eyeshields;Gloves
Hazard Codes N: Dangerous for the environment;Xn: Harmful;
Risk Phrases 51/53-36/37/38-20/21/22
Safety Phrases 61-36-26
RIDADR UN 3077 9/PG 3
RTECS UA8670000
HS Code 2933990090
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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