DC Chemicals Limited
China
Product Name: Celiprolol hydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

57470-78-7

57470-78-7 structure

Name: Celiprolol HCl
Chemical Name: Celiprolol Hydrochloride
CAS Number: 57470-78-7
Molecular Formula: C₂₀H₃₄ClN₃O₄
Molecular Weight: 415.955
Catalog: API Circulatory system medication Antiarrhythmic drug
Create Date: 2018-09-10 20:28:19
Modify Date: 2024-01-02 09:37:48
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].

Name	Celiprolol Hydrochloride
Synonyms	MFCD00941500 3-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-1,1-diethylurea hydrochloride (1:1) Urea, N'-[3-acetyl-4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-N,N-diethyl-, hydrochloride (1:1) (+)-3-(3-Acetyl-4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-1,1-diethylurea hydrochloride Celiprolol Hydrochloride UNII:G1M3398594 3-(3-Acetyl-4-{2-hydroxy-3-[(2-methyl-2-propanyl)amino]propoxy}phenyl)-1,1-diethylurea hydrochloride (1:1) EINECS 260-752-2 Celiprolol HCl 3-[3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-1,1-diethylurea,hydrochloride

Description	Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity[1].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Target	β1-andrenoceptor[1]
In Vivo	Celiprolol (5 or 50 mg/kg; p.o. every day for 12 weeks) has a moderate antihypertensive action at the dose of 50 mg/kg, and significantly reduces media smooth muscle hypertrophy of the mesenteric artery in SHR[2]. Animal Model: Male spontaneously hypertensive rats (SHR) and age-matched Wistar-Kyoto (WKY) rats (8 weeks old)[2] Dosage: 5, 50 mg/kg Administration: P.o. every day (administered in drinking water) for 12 weeks Result: Attenuated the rise in blood pressure significantly at the dose of 50 mg/kg in SHR. Did not significantly affect absolute heart or body weights. Reduced the average medial thickness of the mesenteric artery in SHR.
References	[1]. Nawarskas JJ, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253. [2]. Tolvanen JP, et, al. Effect of celiprolol therapy on arterial dilatation in experimental hypertension. Br J Pharmacol. 1996 Nov; 119(6): 1137-44.

Density	1.114g/cm3
Boiling Point	586.5ºC at 760 mmHg
Melting Point	197-200ºC (dec.)
Molecular Formula	C₂₀H₃₄ClN₃O₄
Molecular Weight	415.955
Flash Point	308.5ºC
Exact Mass	415.223785
PSA	94.39000
LogP	4.09720
Storage condition	Refrigerator

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YR6560000

CHEMICAL NAME :: Urea, 3-(3-acetyl-4-(3-((1,1-dimethylethyl)amino)-2-hydroxy propoxy)phenyl)-1,1-d iethyl-, monohydrochloride

CAS REGISTRY NUMBER :: 57470-78-7

LAST UPDATED :: 199709

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C20-H33-N3-O4.Cl-H

MOLECULAR WEIGHT :: 416.02

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 40 mg/kg/2W-I

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 26,842,1992

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2157 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 754 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 68300 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1362 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 310 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42300 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 512 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 38,443,1989

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 33,41,1983

56980-93-9

~80%

57470-78-7

Literature: Ji, Li; Qian, Chao; Chen, Xin-Zhi; Mao, Xiao-Yuan 2011 , vol. 35, # 11 p. 640 - 643,4

830-03-5

57470-78-7

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100-02-7

57470-78-7

Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178

1450-76-6

57470-78-7

Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178

329722-31-8

57470-78-7

Literature: Organic Process Research and Development, , vol. 5, # 2 p. 176 - 178

1357457-94-3

57470-78-7

Literature: , vol. 35, # 11 p. 640 - 643,4

79881-89-3

57470-78-7

Literature: , vol. 35, # 11 p. 640 - 643,4

100-00-5

57470-78-7

Literature: , vol. 35, # 11 p. 640 - 643,4

13871-68-6

57470-78-7

Literature: , vol. 35, # 11 p. 640 - 643,4

Precursor 8
56980-93-9 830-03-5 100-02-7 1450-76-6
329722-31-8 79881-89-3 100-00-5 13871-68-6
DownStream 0

57470-78-7	56980-93-9
149825-34-3	1700663-41-7
2711717-77-8	111616-54-7
31884-77-2	132539-07-2
15687-41-9	60189-97-1
2012013-34-0	1158522-08-7
2172012-09-6	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4