Dilazep HCl | CAS#20153-98-4 | coronary vasodilator

Dilazep HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 598179

CAS#: 20153-98-4

Description: Dilazep HCl is a coronary vasodilator with some antiarrhythmic activity.

Chemical Structure

Dilazep HCl

CAS# 20153-98-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 598179
Name: Dilazep HCl
CAS#: 20153-98-4
Chemical Formula: C31H46Cl2N2O10
Exact Mass: 0.00
Molecular Weight: 677.613
Elemental Analysis: C, 54.95; H, 6.84; Cl, 10.46; N, 4.13; O, 23.61

Price and Availability

Size	Price	Availability
50mg	USD 550	2 Weeks
100mg	USD 950	2 Weeks
200mg	USD 1650	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 3650	2 Weeks
2g	USD 5950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Dilazep dihydrochloride; Dilazep HCl; AS 05; ASTA C 4898; K-285; K 285; K285;

IUPAC/Chemical Name: (1,4-diazepane-1,4-diyl)bis(propane-3,1-diyl) bis(3,4,5-trimethoxybenzoate) dihydrochloride

InChi Key: VILIWRRWAWKXRW-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H44N2O10.2ClH/c1-36-24-18-22(19-25(37-2)28(24)40-5)30(34)42-16-8-12-32-10-7-11-33(15-14-32)13-9-17-43-31(35)23-20-26(38-3)29(41-6)27(21-23)39-4;;/h18-21H,7-17H2,1-6H3;2*1H

SMILES Code: O=C(OCCCN1CCN(CCCOC(C2=CC(OC)=C(OC)C(OC)=C2)=O)CCC1)C3=CC(OC)=C(OC)C(OC)=C3.[H]Cl.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	Dilazep dihydrochloride is an inhibitor of adenosine uptake.
In vitro activity:	Therefore, these observations may suggest that the suppression of NO synthesis after dilazep treatment in RAW 264 cells is caused by the inhibition of TNF-alpha expression via adenosine receptors. Reference: J Pharmacol Sci. 2010;113(3):271-5. https://pubmed.ncbi.nlm.nih.gov/20647687/
In vivo activity:	Dilazep has been reported to inhibit edema formation in cerebral ischemia model of spontaneously hypertensive rats. These results suggest that dilazep prevents the ischemic damage of BBB, which may contribute to reduction of the brain edema. Reference: Naunyn Schmiedebergs Arch Pharmacol. 1992 Apr;345(4):485-8. https://pubmed.ncbi.nlm.nih.gov/1620248/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Water	100.0	147.58

Preparing Stock Solutions

The following data is based on the product molecular weight 677.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	2. Nakatsuka R, Nozaki T, Shinohara M, Ohura K. Dilazep decreases lipopolysaccharide-induced nitric oxide and TNF-alpha synthesis in RAW 264 cells. J Pharmacol Sci. 2010;113(3):271-5. doi: 10.1254/jphs.09286sc. PMID: 20647687.1. Kawagoe J, Abe K, Ikuta J, Igarashi N, Shimizu S, Yamauchi Y, Kogure K. Effect of dilazep dihydrochloride against ischemia and reperfusion-induced disruption of blood-brain barrier in rats: a quantitative study. Naunyn Schmiedebergs Arch Pharmacol. 1992 Apr;345(4):485-8. doi: 10.1007/BF00176629. PMID: 1620248. 3. Zhang Y, Legare DJ, Geiger JD, Lautt WW. Dilazep potentiation of adenosine-mediated superior mesenteric arterial vasodilation. J Pharmacol Exp Ther. 1991 Sep;258(3):767-71. PMID: 1890619.
In vitro protocol:	1. Nakatsuka R, Nozaki T, Shinohara M, Ohura K. Dilazep decreases lipopolysaccharide-induced nitric oxide and TNF-alpha synthesis in RAW 264 cells. J Pharmacol Sci. 2010;113(3):271-5. doi: 10.1254/jphs.09286sc. PMID: 20647687.
In vivo protocol:	1. Kawagoe J, Abe K, Ikuta J, Igarashi N, Shimizu S, Yamauchi Y, Kogure K. Effect of dilazep dihydrochloride against ischemia and reperfusion-induced disruption of blood-brain barrier in rats: a quantitative study. Naunyn Schmiedebergs Arch Pharmacol. 1992 Apr;345(4):485-8. doi: 10.1007/BF00176629. PMID: 1620248. 2. Zhang Y, Legare DJ, Geiger JD, Lautt WW. Dilazep potentiation of adenosine-mediated superior mesenteric arterial vasodilation. J Pharmacol Exp Ther. 1991 Sep;258(3):767-71. PMID: 1890619.

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1: Pirani R, Gruppillo P. Il dilazep [Dilazep]. G Ital Cardiol. 1980;10(10):1419-25. Italian. PMID: 7016654.

2: Deguchi H, Takeya H, Wada H, Gabazza EC, Hayashi N, Urano H, Suzuki K. Dilazep, an antiplatelet agent, inhibits tissue factor expression in endothelial cells and monocytes. Blood. 1997 Sep 15;90(6):2345-56. PMID: 9310485.

3: Zeng H, Liu S, Wang P, Qu X, Ji H, Wang X, Zhu X, Song Z, Yang X, Ma Z, Zhu H. Dilazep synergistically reactivates latent HIV-1 in latently infected cells. Mol Biol Rep. 2014 Nov;41(11):7697-704. doi: 10.1007/s11033-014-3662-z. Epub 2014 Aug 5. PMID: 25091947.

4: Nakatsuka R, Nozaki T, Shinohara M, Ohura K. Dilazep decreases lipopolysaccharide-induced nitric oxide and TNF-alpha synthesis in RAW 264 cells. J Pharmacol Sci. 2010;113(3):271-5. doi: 10.1254/jphs.09286sc. PMID: 20647687.

5: Playa H, Lewis TA, Ting A, Suh BC, Muñoz B, Matuza R, Passer BJ, Schreiber SL, Buolamwini JK. Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). Bioorg Med Chem Lett. 2014 Dec 15;24(24):5801-5804. doi: 10.1016/j.bmcl.2014.10.026. Epub 2014 Oct 28. PMID: 25454272; PMCID: PMC5695681.

6: Tonini M, Perucca E, Manzo L, Marcoli M, D'Angelo L, Saltarelli P, Onori L. Dilazep: an inhibitor of adenosine uptake with intrinsic calcium antagonistic properties. J Pharm Pharmacol. 1983 Jul;35(7):434-9. doi: 10.1111/j.2042-7158.1983.tb04317.x. PMID: 6136584.

7: Sonoki K, Iwase M, Iino K, Ichikawa K, Yoshinari M, Ohdo S, Higuchi S, Iida M. Dilazep and fenofibric acid inhibit MCP-1 mRNA expression in glycoxidized LDL-stimulated human endothelial cells. Eur J Pharmacol. 2003 Aug 15;475(1-3):139-47. doi: 10.1016/s0014-2999(03)02109-5. PMID: 12954370.

8: Sakumura T, Fujii Z, Umemoto S, Murakami T, Kawata Y, Fujii K, Minami M, Sasaki K, Matsuzaki M. Dilazep, a nucleoside transporter inhibitor, modulates cell cycle progression and DNA synthesis in rat mesangial cells in vitro. Cell Prolif. 2000 Feb;33(1):19-28. doi: 10.1046/j.1365-2184.2000.00145.x. PMID: 10741641; PMCID: PMC6622404.

9: Gohda T, Makita Y, Shike T, Funabiki K, Shirato I, Tomino Y. Dilazep hydrochloride, an antiplatelet drug, inhibits lipopolysaccharide-induced mouse mesangial cell IL-6 secretion and proliferation. Kidney Blood Press Res. 2001;24(1):33-8. doi: 10.1159/000054203. PMID: 11174004.

10: Kawabata M, Haneda M, Wang T, Imai M, Takabatake T. Effects of a nucleoside transporter inhibitor, dilazep, on renal microcirculation in rats. Hypertens Res. 2002 Jul;25(4):615-21. doi: 10.1291/hypres.25.615. PMID: 12358150.

11: Zhang Y, Legare DJ, Geiger JD, Lautt WW. Dilazep potentiation of adenosine- mediated superior mesenteric arterial vasodilation. J Pharmacol Exp Ther. 1991 Sep;258(3):767-71. PMID: 1890619.

12: Zhou H. Dilazep and dipyridamole inhibit tissue factor expression on monocytes induced by IgG from patients with antiphospholipid syndrome. Acta Pharmacol Sin. 2004 Oct;25(10):1366-71. PMID: 15456541.

13: Haga N, Miura I, Fujisawa Y, Fukushi Y, Abiko Y. Effect of dilazep on decrease in myocardial pH during ischemia in dogs. Arzneimittelforschung. 1986 Jun;36(6):913-6. PMID: 3741523.

14: Marzilli M, Trivella MG, Levantesi D, Pelosi G, Dalle Vacche M, Taddei L, L'Abbate A. Effect of dilazep on coronary and systemic circulations. Pharmacology. 1985;31(2):82-7. doi: 10.1159/000138102. PMID: 4023048.

15: Chiba K, Hashizume H, Inagaki SI, Abiko Y. Dilazep inhibits binding of batrachotoxin to sodium channels in canine sarcolemmal vesicles. Arch Int Pharmacodyn Ther. 1995 Sep-Oct;330(2):138-50. PMID: 8861708.

16: Fujita S, Ishida Y, Izumi K, Moritoki H, Ohara M, Takei M. Potentiation by dilazep on the negative inotropic effect of adenosine on guinea-pig atria. Br J Pharmacol. 1980 Feb;68(2):343-9. doi: 10.1111/j.1476-5381.1980.tb10423.x. PMID: 7357212; PMCID: PMC2043930.

17: Poggesi L, Masotti G, Serneri GG, Carnovali M. Intravenous dilazep reduces blood pressure and peripheral vascular resistance in humans. J Clin Pharmacol. 1988 Jan;28(1):43-7. doi: 10.1002/j.1552-4604.1988.tb03099.x. Erratum in: J Clin Pharmacol 1988 Apr;28(4):326. PMID: 3280614.

18: Thorn JA, Jarvis SM. Adenosine transporters. Gen Pharmacol. 1996 Jun;27(4):613-20. doi: 10.1016/0306-3623(95)02053-5. PMID: 8853292.

19: Persson P, Fasching A, Pihl L, Palm F. Adenosine reuptake inhibition reduces diabetes-induced glomerular hyperfiltration via the adenosine A2a receptor. Am J Physiol Regul Integr Comp Physiol. 2023 Oct 1;325(4):R337-R343. doi: 10.1152/ajpregu.00278.2022. Epub 2023 Jul 24. PMID: 37486069.

20: Gati WP, Paterson AR. Interaction of [3H]dilazep at nucleoside transporter- associated binding sites on S49 mouse lymphoma cells. Mol Pharmacol. 1989 Jul;36(1):134-41. PMID: 2747624.

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