Description | Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist). | ||||||||||||
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Related Catalog |
Signaling Pathways
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Membrane Transporter/Ion Channel
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Calcium Channel
Research Areas
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Cardiovascular Disease
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In Vitro | Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels[1]. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K+ and a low concentration of norepinephrine (NE)[2]. Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC50 of 10-20 μM)[3]. | ||||||||||||
In Vivo | Diltiazem produces a noncompetitive inhibition of Ca2+-induced contractions of depolarized rabbit aorta. Furthermore, there is a lack of parallelism between the smooth muscle effects of removal of [Ca2+]ex and of addition of diltiazem[2]. Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. The treatment of hyperthyroid rats with losartan diltiazem (4.7±0.7%; P < 0.001) significantly reduces the percentage of fibrosis areas in the left ventricle [4]. In conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreases the blood pressure and increases the heart rate after intravenous administration (0.03--1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduces the blood pressure of SHR[5]. | ||||||||||||
Solvent |
In Vitro:
H 2 O : 33.33 mg/mL (73.91 mM; Need ultrasonic) |
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Solubility |
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Storage |
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Shipping | Room temperature in continental US; may vary elsewhere | ||||||||||||
SMILES | CN(C)CCN1C2=CC=CC=C2S[@H](C3=CC=C(OC)C=C3)[@H](OC(C)=O)C1=O.Cl | ||||||||||||
References |
[1]. Kraus RL, et al. Molecular mechanism of diltiazem interaction with L-type Ca2+ channels. J Biol Chem. 1998 Oct 16;273(42):27205-12. [2]. van Breemen C, et al. The mechanism of inhibitory action of diltiazem on vascular smooth muscle contractility. J Pharmacol Exp Ther. 1981 Aug;218(2):459-63. [3]. Chiesi M, et al. Stereospecific action of diltiazem on the mitochondrial Na-Ca exchange system and on sarcolemmal Ca-channels. Biochem Pharmacol. 1987 Sep 1;36(17):2735-40. [4]. Freitas F, et al. Cardiac microvascular rarefaction in hyperthyroid rats is reversed by losartan, diltiazem. Fundam Clin Pharmacol. 2015 Feb;29(1):31-40. [5]. Sato M, et al. Hypotensive effects of diltiazem hydrochloride in the normotensive, spontaneously hypertensive and renal hypertensive rats (author's transl). Nihon Yakurigaku Zasshi. 1979 Mar;75(2):99-106. |
Density | 1.26g/cm3 |
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Boiling Point | 594.4ºC at 760mmHg |
Melting Point | 212-214 °C |
Molecular Formula | C 22 H 27 ClN 2 O 4 S |
Molecular Weight | 450.979 |
Flash Point | 313.3ºC |
Exact Mass | 450.138000 |
PSA | 84.38000 |
LogP | 4.23550 |
Index of Refraction | 118 ° (C=1, H2O) |
Storage condition | 2-8°C |
Water Solubility | soluble |
Name | CAS | Appearance |
Ethyl 2-phenylacetoacetate | 5413-05-8 | White powder |
Diethyl(phenylacetyl)malonate | 20320-59-6 | White powder |
BMK methyl glycidate | 80532-66-7 | Yellow liquid |
3-OXO-4-PHENYL-BUTYRIC ACID ETHYL ESTER | 718-08-1 | Clear liquid |
1-(benzo[d][1,3]dioxol-5-yl)-2-bromopropan-1-one | 52190-28-0 | Brown powder |
PMK ethyl glycidate | 28578-16-7 | Brown liquid |
2-Benzylamino-2-methyl-1-propanol | 10250-27-8 | White powder |
2-iodo-1-p-tolyl-propan-1-one | 236117-38-7 | Yellow powder |
1-(Benzyloxycarbonyl)-4-piperidinone | 19099-93-5 | White powder |
1-BOC-4-(4-FLUORO-PHENYLAMINO)-PIPERIDINE | 288573-56-8 | White powder |
1-BOC-4-(4-BROMO-PHENYLAMINO)-PIPERIDINE | 443998-65-0 | White powder |
1-Phenyl-2-nitropropene | 705-60-2 | Yellow diamond crystal |
docosyltrimethylammonium methyl sulphate | 81646-13-1 | White flake |
2-Amino-4-phenylbutane | 22374-89-6 | Transparent crystal |
Tetramisole hydrochloride | White powder Contained crystal | |
N-Isopropylbenzylamine | 102-97-6 | Clear crystal pink blue |
Valerophenone | 1009-14-9 | Clear liquid or Yellow liquid |
4'-Methylpropiophenone | 5337-93-9 | Clear liquid or Yellow liquid |
Tryptamine | 61-54-1 | White powder |
Dimethyl terephthalate | 120-61-6 | Colorless rhombic crystal system crystal |
Valerophenone | 1009-14-9 | White liquid |
N-(2,6-Dimethylphenl)-2-Piperidine Carboxamide | 15883-20-2 | White powder |
4-Methylpropiophenone | 5337-93-9 | Yellow liquid |
Benzylisopropylamine | 102-97-6 | Transparent crystal, transparent column, pink, blue |
5-Nitro-2-(bromoacetamido)benzophenone | 2011-70-3 | |
Nitazoxanide | 55981-09-4 | White powder |
1H-Indole-5,6-diol | 3131-52-0 | White powder |
D-Tartaric acid | 147-71-7 | White powder |
L-(+)-Tartaric acid | 526-83-0 | White powder |
L(+)-Tartaric acid | 87-69-4 | White powder |
DL-Tartaric acid | 133-37-9 | White powder |
1-Boc-3-Piperidinone | 98977-36-7 | Yellow powder |
tert-butyl 4-(4-bromoanilino)piperidine-1-carboxylate | 443998-65-0 | White powder |
tert-butyl 4-(4-fluoroanilino)piperidine-1-carboxylate | 288573-56-8 | White powder |
N-Benzyl-4-piperidone | 3612-20-2 | Yellow liquid |
4-oxopiperidinium chloride | 41979-39-9 | Yellow powder |
N-Phenyl-4-biphenylamine | 32228-99-2 | White powder |
N-BOC-aniline | 3422/1/3 | White powder |
4'-Methoxypropiophenone | 121-97-1 | White powder |
2-iodo-1-p-tolylpropan-1-one | 236117-38-7 | Yellow powder |
2-bromo-1-phenylhexan-1-one | 59774-06-0 | Yellow liquid |
2-iodo-1-phenyl-pentane-1-one | 124878-55-3 | Yellow liquid |
hexanophenone | 942-92-7 | White liquid |
2-(2-chlorophenyl)cyclohexan-1-one | 91393-49-6 | Yellow liquid |
2-Oxiranecarboxylicacid, 3-(1,3-benzodioxol-5-yl)-2-methyl-, ethyl ester | 28578-16-7 | Yellow liquid,Yellow powder,White powder |
1-Bromocyclopentyl-o-chlorophenyl ketone | White powder | |
Nicotinamide riboside chloride | 23111-00-4 | White powder |
1,4-Dimethoxy-2-(2-nitroethenyl) benzene | 40276-11-7 | Brown red color,White powder |
1-Phenyl-2-nitropropene | 705-60-2 | Yellow powder |
Loperamide hydrochloride | 34552-83-5 | White powder |
N-Benzyl-4-piperidone | 3612-20-2 | Yellow liquid |
1-Boc-3-Piperidinone | 98977-36-7 | Yellow powder |
Diethyl(phenylacetyl)malonate | 20320-59-6 | Brown red liquid |
(2S)-2-Ethylbutyl 2-(((perfluorophenoxy)(phenoxy)phosphoryl)amino)propanoate | 1911578-98-7 | White powder |
Tetramisole hydrochloride | White powder | |
Piperidin-4-one hydrochloride | 41979-39-9 | White powder |
5-(2-Fluorophenyl)-1H-pyrrole-3-carbonitrile | 1240948-77-9 | White powder |
5-(2-Fluorophenyl)-1H-pyrrole-3-carbaldehyde | 881674-56-2 | White powder |
5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrole-3-carbaldehyde | 881677-11-8 | White powder |
Pyridine-3-sulfonyl chloride | 16133-25-8 | White powder |
1-Boc-3-piperidone | 98977-36-7 | Yellow powder |
(R)-7-(Benzyloxy)-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione | 1985607-70-2 | White powder |
Loperamide hydrochloride | 34552-83-5 | White powder |
3-Benzyloxy-4-oxo-4H-pyran-2-carboxylic acid | 119736-16-2 | White powder |
methyl-2-methyl-3-phenylglycidate | 80532-66-7 | White powder |
N-Carbethoxy-4-piperidone | 29976-53-2 | Yellow liquid |
N-[(S)-(4-nitrophenoxy)phenoxyphosphinyl]-L-Alanine 2-ethylbutyl ester | 1354823-36-1 | White powder |
Benzyl alcohol | 100-51-6 | White liquid,White powder |
2-Bromo-4-fluoroaniline | 1003-98-1 | Yellow liquid |
Albendazole | 54965-21-8 | White powder |
Cysteamine Hydrochloride | 156-57-0 | White powder |
Olmesartan medoxomil | 144689-63-4 | White powder |
Florfenicol | 76639-94-6 | White powder |
Sulfanilamide | 63-74-1 | White grain |
Nafamostat mesylate | 82956-11-4 | White powder |
Dexmedetomidine | 113775-47-6 | White powder |
Bromadol | 77239-98-6 | White powder |
Cedrol | 77-53-2 | White powder |
Ferrous sulfate heptahydrate | 7782-63-0 | Light green powder |
1-Bromo-3,5-dimethyladamantane | 941-37-7 | Clear liquid |
1,3-Dimethyladamantane | 702-79-4 | Clear liquid |
docosyl-trimethyl-azanium; sulfonatooxymethane | 81646-13-1 | White flake |
Anethole | 4180-23-8 | Clear liquid |
3-Amino-1-hydroxyadamantane | 702-82-9 | White powder |
Furosemide | 54-31-9 | White powder |
2-Piperidone | 675-20-7 | White powder |
Levobupivacaine hydrochloride | 27262-48-2 | White powder |
8-ETHYL-5,8-DIHYDRO-5-OXO-2-[1-PIPERAZINYL]PYRIDO[2,3-D]-PYRIMIDINE-6-CARBOXYLIC ACID | 51940-44-4 | White powder |
Dihydroxyacetone (1,3-Dihydroxyacetone) | 96-26-4 | White powder |
Denatonium | 3734-33-6 | White powder |
Benzoate | 532-32-1 | White powder |
2-ethylhexanol | 104-76-7 | White powder,Clear liquid |
Cesium chloride (Caesium chloride) | 7647-17-8 | White powder |