CAS 123524-52-7|Azelnidipine
| Common Name | Azelnidipine | ||
|---|---|---|---|
| CAS Number | 123524-52-7 | Molecular Weight | 582.646 |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 709.3±60.0 °C at 760 mmHg |
| Molecular Formula | C33H34N4O6 | Melting Point | 120-126ºC |
| MSDS | ChineseUSA | Flash Point | 382.8±32.9 °C |
| Symbol | GHS05, GHS07 | Signal Word | Danger |
Names
| Name | Azelnidipine |
|---|---|
| Synonym | More Synonyms |
Azelnidipine BiologicalActivity
| Description | Azelnidipine(CS 905; Calblock) is a novel dihydropyridine derivative, a L-type calcium channel blocker, and an antihypertensive.IC50 value:Target: L-type calcium channelAcute administration of azelnidipine prevents a sudden drop of cardiac function after acute stress. Azelnidipine may have a protective role in inflammation associated with atherosclerosis. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>Calcium ChannelResearch Areas >>Cardiovascular Disease |
| References | [1]. Komoda H, Inoue T, Node K. Anti-inflammatory properties of azelnidipine, a dihydropyridine-based calcium channel blocker. Clin Exp Hypertens. 2010 Jan;32(2):121-8. [2]. Kain V, Kumar S, Sitasawad SL. Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis. Cardiovasc Diabetol. 2011 Nov 4;10:97. [3]. Takano Y, Ueyama T, Ishikura F. Azelnidipine, unique calcium channel blocker could prevent stress-induced cardiac dysfunction like α·β blocker. J Cardiol. 2012 Jul;60(1):18-22. [4]. Shimizu T, Tanaka T, Iso T et al. Azelnidipine inhibits MSX2-dependent osteogenic differentiation and matrix mineralization of vascular smooth muscle cells. Int Heart J. 2012;53(5):331-5. [5]. Ohyama T, Sato K, Kishimoto K et al. Azelnidipine is a calcium blocker that attenuates liver fibrosis and may increase antioxidant defence. Br J Pharmacol. 2012 Feb;165(4b):1173-87. |
Chemical & Physical Properties
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 709.3±60.0 °C at 760 mmHg |
| Melting Point | 120-126ºC |
| Molecular Formula | C33H34N4O6 |
| Molecular Weight | 582.646 |
| Flash Point | 382.8±32.9 °C |
| Exact Mass | 582.247864 |
| PSA | 139.71000 |
| LogP | 4.21 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.659 |
| InChIKey | ZKFQEACEUNWPMT-UHFFFAOYSA-N |
| SMILES | CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1 |
| Storage condition | Room temp |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 3640 mg/kg/1Y-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - urine volume increased Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - changes in chlorine
- 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: 25,1757,1997
Safety Information
| Symbol | GHS05, GHS07 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H302-H318 |
| Precautionary Statements | P280-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xn |
| Risk Phrases | R22 |
| Safety Phrases | 26-39 |
| RIDADR | NONH for all modes of transport |
| RTECS | US7968332 |
| HS Code | 2933990090 |
Customs
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Articles32
More Articles| Anti-atherogenic effects of the combination therapy with olmesartan and azelnidipine in diabetic apolipoprotein E-deficient mice. Tohoku J. Exp. Med. 228 , 305-315, (2012) Many studies have aimed to identify anti-atherogenic agents in cardiovascular medicine. We have recently demonstrated that the combination therapy with olmesartan (OLM), an angiotensin II receptor blo... | |
| The pharmacological differences in antianginal effects of long-lasting calcium channel blockers: azelnidipine and amlodipine. J. Cardiovasc. Pharmacol. 61(1) , 63-9, (2013) We examined antianginal effects of azelnidipine and amlodipine in an arginine vasopressin-induced rat anginal model. Oral administration of azelnidipine or amlodipine produced long lasting inhibition ... | |
| Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis. Cardiovasc. Diabetol. 10 , 97, (2011) Numerous evidences suggest that diabetic heart is characterized by compromised ventricular contraction and prolonged relaxation attributable to multiple causative factors including calcium accumulatio... |
Synonyms
| Azelnidipine |
| 3-[1-(Diphenylmethyl)-3-azetidinyl] 5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate |
| 3-[1-(Diphenylmethyl)azetidin-3-yl] 5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| UNII:PV23P19YUG |
| 3,5-Pyridinedicarboxylic acid (2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl) |
| 3-[1-(diphenylmethyl)azetidin-3-yl] 5-propan-2-yl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| 3-O-(1-benzhydrylazetidin-3-yl) 5-O-propan-2-yl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| (±)-1,4-Dihydro-2-amino-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic Acid 3-(1-(Diphenylmethyl)-3-azetidinyl) 5-(1-Methylethyl) Ester |
| 3,5-Pyridinedicarboxylic acid, 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-, 3-[1-(diphenylmethyl)-3-azetidinyl] 5-(1-methylethyl) ester |
| 3-(1-(Diphenylmethyl)-3-azetidinyl) 5-Isopropyl (±)-2-Amino-1,4-dihydro-6-methyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| MFCD00865803 |
