DC Chemicals Limited
China
Product Name: Lacidipine
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Purity: 98.0%
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Henan Tianfu Chemical Co., Ltd.
China
Product Name: Lacidipine, 99%
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Purity: 99.0%
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103890-78-4

103890-78-4 structure

Name: Lacidipine
Chemical Name: diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate
CAS Number: 103890-78-4
Molecular Formula: C₂₆H₃₃NO₆
Molecular Weight: 455.543
Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
Create Date: 2018-02-16 08:00:00
Modify Date: 2024-01-01 19:18:57
Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker. Target: Calcium ChannelLacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway [1]. In biological membranes deriving from rat brain tissue, lacidipine showed an activity comparable to reference antioxidant compounds like vitamin E [2]. lacidipine has some important protective effects on liver of hypertensive irradiated albino rats [3].

Name	diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate
Synonyms	Caldine Diethyl 2,6-dimethyl-4-(2-{(1E)-3-[(2-methyl-2-propanyl)oxy]-3-oxo-1-propen-1-yl}phenyl)-1,4-dihydro-3,5-pyridinedicarboxylate 4-[o-[(E)-2-Carboxyvinyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid 4-tert-Butyl Diethyl Ester Diethyl 4-{2-[(1E)-3-tert-butoxy-3-oxoprop-1-en-1-yl]phenyl}-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate Diethyl (E)-4-[2-[2-(tert-butoxycarbonyl)vinyl]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate Lacipil (E)-4-[2-[3-(1,1-Dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester MFCD00865936 Lacirex 3,5-Pyridinedicarboxylic acid, 4-[2-[(1E)-3-(1,1-dimethylethoxy)-3-oxo-1-propen-1-yl]phenyl]-1,4-dihydro-2,6-dimethyl-, diethyl ester Lacidipine Motens

Description	Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker. Target: Calcium ChannelLacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway [1]. In biological membranes deriving from rat brain tissue, lacidipine showed an activity comparable to reference antioxidant compounds like vitamin E [2]. lacidipine has some important protective effects on liver of hypertensive irradiated albino rats [3].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
References	[1]. Zhang, A., et al., Lacidipine attenuates apoptosis via a caspase-3 dependent pathway in human kidney cells. Cell Physiol Biochem, 2013. 32(4): p. 1040-9. [2]. van Amsterdam, F.T., et al., Lacidipine: a dihydropyridine calcium antagonist with antioxidant activity. Free Radic Biol Med, 1992. 12(3): p. 183-7. [3]. Kamal, S.M., Possible hepatoprotective effects of lacidipine in irradiated DOCA-salt hypertensive albino rats. Pak J Biol Sci, 2013. 16(21): p. 1353-7.

Density	1.1±0.1 g/cm3
Boiling Point	558.4±50.0 °C at 760 mmHg
Melting Point	174-175°C
Molecular Formula	C₂₆H₃₃NO₆
Molecular Weight	455.543
Flash Point	291.5±30.1 °C
Exact Mass	455.230774
PSA	90.93000
LogP	5.49
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.540
Storage condition	-20?C Freezer

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US7970200

CHEMICAL NAME :: 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-(3-(1,1-dimethylethoxy) -3-oxo-1- propenyl)phenyl)-, diethyl ester, (E)-

CAS REGISTRY NUMBER :: 103890-78-4

LAST UPDATED :: 199410

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C26-H33-N-O6

MOLECULAR WEIGHT :: 455.60

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 :: 880 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 43300 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 562 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3150 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 80200 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Skin and Appendages - hair

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,335,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 291 mg/kg/1Y-I

TOXIC EFFECTS :: Cardiac - EKG changes not diagnostic of specified effects Endocrine - changes in adrenal weight Endocrine - changes in thymus weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,343,1994 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1260 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 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 - fetal death

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,377,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 52 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,399,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 234 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,389,1994

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Hazard Codes	C,Xi
Risk Phrases	R20/21/22
Safety Phrases	S26-S36/37/39-S45
RIDADR	UN 3265 8/PG 2
WGK Germany	3
Packaging Group	III
Hazard Class	8
HS Code	2933399090

59159-39-6

626-34-6

643-79-8

~41%

103890-78-4

Literature: Sajja, Eswaraiah; Vetukuri, Venkata Naga Kali Vara Prasada Raju; Ningam, Srinivas Reddy; Vedantham, Ravindra Patent: US2007/43088 A1, 2007 ; Location in patent: Page/Page column 6 ;

103890-69-3

144-55-8

626-34-6

103890-78-4

Literature: US4801599 A1, ;

Precursor 5
59159-39-6 626-34-6 643-79-8 103890-69-3
144-55-8
DownStream 0

HS Code	2933399090
Summary	2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

103890-78-4	1185245-62-8
103890-79-5	1261432-01-2
1217211-78-3	103890-81-9