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246852-12-0

246852-12-0 structure
246852-12-0 structure
  • Name: Norvasc
  • Chemical Name: 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate,methanesulfonic acid
  • CAS Number: 246852-12-0
  • Molecular Formula: C21H29ClN2O8S
  • Molecular Weight: 504.982
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
  • Create Date: 2018-06-30 20:29:24
  • Modify Date: 2024-01-09 17:08:42
  • Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].

Name 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate,methanesulfonic acid
Synonyms 3,5-Pyridinedicarboxylic acid, 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester, methanesulfonate (1:1)
3-Ethyl 5-methyl 2-((2-aminoethoxy)methyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate methanesulfonate
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate methanesulfonate (1:1)
Norvasc
UNII-291Y33EZHA
Amlodipine Mesilate
Amlodipine Mesylate
UNII:291Y33EZHA
3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate methanesulfonate (1:1)
Description Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].
Related Catalog
Target

L-type calcium channel

In Vitro Amlodipine mesylate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3]. Amlodipine mesylate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3]. Amlodipine mesylate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].
In Vivo Amlodipine mesylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4]. Amlodipine mesylate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3]. Animal Model: ATP2B1loxP/loxP mice[4] Dosage: 5 mg/kg/day Administration: Subcutaneously implanted osmotic pump for 2 weeks Result: Significantly decreased the blood pressure.
References

[1]. Kishen G. Bulsara, et al. Amlodipine.

[2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

[3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

[4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

Molecular Formula C21H29ClN2O8S
Molecular Weight 504.982
Exact Mass 504.133301
PSA 162.63000
LogP 3.88020
Hazard Codes Xn
HS Code 2933399090
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%