Efonidipine (NZ-105)
(Synonyms: 依福地平,NZ-105; (±)-Efonidipine) 目录号 : GC32580
An L- and T-type calcium channel inhibitor
Cas No.:111011-63-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Efonidipine is an inhibitor of L- and T-type voltage-gated calcium channels (Cavs).1 It inhibits Cav1.2a (IC50 = 1.8 nM for the hamster channel), an L-type Cav, and Cav3.2 (IC50 = 350 nM for the human channel), a T-type Cav. It also inhibits L- and T-type calcium channels and fetal bovine serum-induced hypertrophy in isolated mouse cardiomyocytes.2 Efonidipine (200 mg/kg) increases survival in a mouse model of acute myocardial infarction induced by ligation of the left coronary artery.3 Efonidipine is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro; IC50 = 38.5 nM).4
1.Lee, T.-S., Kaku, T., Takebayashi, S., et al.Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca2+ channels with distinct inhibitory mechanismsPharmacology78(1)11-20(2006) 2.Horiba, M., Muto, T., Ueda, N., et al.T-type Ca2+ channel blockers prevent cardiac cell hypertrophy through an inhibition of calcineurin-NFAT3 activation as well as L-type Ca2+ channel blockersLife Sci.82(11-12)554-560(2008) 3.Kinoshita, H., Kuwahara, K., Takano, M., et al.T-type Ca2+ channel blockade prevents sudden death in mice with heart failureCirculation120(9)743-752(2009) 4.Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al.Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2ACS Med. Chem. Lett.11(12)2526-2533(2020)
| Cas No. | 111011-63-3 | SDF | |
| 别名 | 依福地平,NZ-105; (±)-Efonidipine | ||
| Canonical SMILES | CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1 | ||
| 分子式 | C34H38N3O7P | 分子量 | 631.66 |
| 溶解度 | DMSO: 20 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5831 mL | 7.9157 mL | 15.8313 mL |
| 5 mM | 0.3166 mL | 1.5831 mL | 3.1663 mL |
| 10 mM | 0.1583 mL | 0.7916 mL | 1.5831 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Effects of Efonidipine hydrochloride (NZ-105), a new calcium antagonist, against acute renal failure in rats
Gen Pharmacol 1994 Nov;25(7):1451-8.PMID:7896060DOI:10.1016/0306-3623(94)90173-2.
1. We investigated the effect of Efonidipine hydrochloride (NZ-105) against acute renal failure (ARF) in male Wistar rats. ARF was produced by ischemia or glycerol. 2. Ischemia-induced ARF was produced by right nephrectomy and clamping of the left renal artery for 60 min, followed by reperfusion. NZ-105 (20 mg/kg) was orally administered twice a day for 3 days before ARF. The plasma creatinine and urea nitrogen concentrations were markedly elevated in the ischemia ARF group on the 1st day, but the elevation was significantly suppressed by NZ-105 treatment. 3. Glycerol-induced ARF was produced by intramuscular injection of 50% (v/v) glycerol (10 ml/kg) in rats which were restricted to drinking water for 24 hr. NZ-105 (20 mg/kg) was orally administered twice a day for 3 days before ARF. NZ-105 significantly attenuated the severe impairment of creatinine and urea nitrogen clearances and the elevated fractional sodium excretion (FENa) caused by ARF. 4. In the kidney homogenate, NZ-105 (10(-6)-10(-4) M) inhibited lipid peroxidation induced by ascorbic acid and Fe or by NADPH and the inhibitory effect of NZ-105 was stronger than alpha-tocopherol, an antioxidant agent. NZ-105 (10(-5)-10(-3) M) showed radical scavenging action against diphenyl-p-picrylhydrazyl and galvinoxyl induced radicals. 5. These findings suggest that NZ-105 prevents the renal damage caused by the two kinds of ARF. Moreover, the inhibitory effects of NZ-105 against lipid peroxidation and radical formation may be one of the mechanisms involved in the prevention of ARF.
Renal protective effect of Efonidipine hydrochloride (NZ-105), a new calcium antagonist, in spontaneously hypertensive rats
Gen Pharmacol 1994 Dec;25(8):1567-75.PMID:7721030DOI:10.1016/0306-3623(94)90356-5.
1. We investigated the renal protective effect of Efonidipine hydrochloride (NZ-105) in spontaneously hypertensive rats (SHR). SHR were given a diet containing 0.075% NZ-105 from 8 weeks old for 20 weeks. 2. 24-hr urinary protein excretion in the control SHR (drug-free diet) increased with age (from 77.3 mg/kg/day at 8 weeks old to 385.4 mg/kg/day at 28 weeks old), while that in NZ-105-treated SHR was maintained at almost the same level as that in Wistar-Kyoto rats (WKY), matched control animals throughout the experimental period. 3. The histological changes of the kidney were examined by light microscopy at the end of the treatment period. In control SHR, swelling and hyalinization of glomeruli, dilatation of renal tubules containing hyaline casts and arteriolosclerosis were revealed. The long-term administration of NZ-105 markedly suppressed these changes. 4. The kidney weights and plasma creatinine concentration in control SHR were higher than those in WKY, while they were significantly reduced in NZ-105-treated SHR. The long-term administration of NZ-105 also suppressed the elevation of systolic blood pressure and the increases of plasma renin activity and aldosterone concentration. 5. These findings suggest that NZ-105 inhibits the development of proteinuria and progressive kidney damage in SHR and may become a useful antihypertensive drug with the renal protective effect.
Effects of Efonidipine hydrochloride (NZ-105), a calcium antagonist, on renal function in conscious spontaneously hypertensive rats
Gen Pharmacol 1995 Mar;26(2):333-7.PMID:7590083DOI:10.1016/0306-3623(94)00192-p.
1. We investigated the effects of short- and long-term administration of Efonidipine hydrochloride (NZ-105), 1,4-dihydropyridine derivative, in conscious spontaneously hypertensive rats (SHR). 2. Oral administration of NZ-105 for 12 weeks caused diuretic and natriuretic effects, which were not attenuated during the experimental period. 3. In the short-term experiment for investigating the mechanism of the diuretic effect, intravenous injection of NZ-105 (0.03 mg/kg of body weight) significantly increased the urine volume (UV), renal plasma flow (RPF) and glomerular filtration rate (GFR). The increment rate of UV and RPF was 105.4 +/- 17.8% and 111.7 +/- 72.8%, respectively, which were larger than the increment rate of GFR (38.5 +/- 14.0%). 4. The diuretic or natriuretic effect of NZ-105 was suggested to be due to both the inhibition of sodium reabsorption and, at least in part, the increase of GFR.
Efonidipine-Induced Exanthematic Drug Eruption and Literature Review
J Cardiovasc Pharmacol 2019 Jun;73(6):394-396.PMID:31162248DOI:10.1097/FJC.0000000000000676.
We report the case of an elderly woman who developed exanthematic drug eruption after administration of Efonidipine. An 84-year-old woman presented to emergency department with complaints of generalized itching and erythema since 4 days. She was on human-soluble insulin since 11 years. In view of her hypertension and left anterior descending artery stenosis, she was initiated on aspirin, clopidogrel, atorvastatin, pantoprazole, nebivolol, aldactone, and Efonidipine a week ago. Her presenting complaints were initially managed with parenteral pheniramine maleate and hydrocortisone. She was admitted, and all her medications except antiplatelets and insulin were discontinued. She was prescribed topical beclomethasone and oral antihistamines for better control of her symptoms. To confirm the drug precipitating the reaction, she was rechallenged with Efonidipine, 20 mg once daily on the third day of admission. She developed itching 8 hours after administering the medication, and Efonidipine was stopped and nebivolol 5 mg once daily was restarted for hypertension. She did not develop any adverse event when the remaining medications were reinitiated. World Health Organization-Uppsala Monitoring Centre causality assessment criteria indicated a "certain" association. To the best of the knowledge of the authors, this is one among the first reported cases of efonidipine-induced exanthematic drug eruption.
[Effect of Efonidipine hydrochloride (NZ-105), a dihydropyridine derivative with calcium antagonistic action, on myocardial oxygen tension in anesthetized dogs]
Nihon Yakurigaku Zasshi 1996 Nov;108(5):267-74.PMID:8974087DOI:10.1254/fpj.108.267.
Effect of Efonidipine hydrochloride (Efonidipine) on myocardial oxygen tension (PO2) was investigated in open-chest anesthetized dog and compared with those of nifedipine and nisoldipine. PO2 was measured by a membrane-coated platinum wire, which was inserted into the myocardium. Intravenous administration of Efonidipine (10 and 30 micrograms/kg) decreased mean blood pressure to a similar extent to that induced by nifedipine (1 and 3 micrograms/kg) or nisoldipine (1 and 3 micrograms/kg). Efonidipine increased coronary blood flow (CBF) and decreased the double product (DP) dose-dependently. Similar results were observed in nisoldipine-treated animals. Nifedipine produced a transient increase in CBF and a transient decrease in DP. The duration of action of Efonidipine on CBF was longer than that of nifedipine or nisoldipine. Efonidipine increased PO2, and the effect was more pronounced in the endocardial region than in the epicardial region. Nifedipine had no significant effect on the PO2, while nisoldipine significantly increased PO2 in the endocardial region. The effect of Efonidipine on the PO2 was greater than that of nisoldipine and the duration of action of Efonidipine was longer than that of nisoldipine. These results suggest that Efonidipine may increase PO2 by mediating, at least in part, a long-lasting increase in oxygen supply and a decrease in oxygen demand in dog heart.