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103890-78-4

103890-78-4 structure
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: 2025-08-21 12:46:50
  • 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
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
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 structure

59159-39-6

626-34-6 structure

626-34-6

643-79-8 structure

643-79-8

~41%

103890-78-4 structure

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 structure

103890-69-3

144-55-8 structure

144-55-8

626-34-6 structure

626-34-6

~%

103890-78-4 structure

103890-78-4

Literature: US4801599 A1, ;
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%
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