Siramesine hydrochloride - CAS 224177-60-0
Catalog number: 224177-60-0
Category: Inhibitor
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Molecular Formula:
C30H32ClFN2O
Molecular Weight:
491.04
COA:
Inquire
Targets:
Sigma Receptor
Description:
Siramesine hydrochloride is the hydrochloride salt form of Siramesine. Siramesine is a selective sigma-2 receptor agonist with a potent anticancer activity in vivo. It was originally devevloped for treating depressant and it has pro-apoptotic activity on
Related CAS:
147817-50-3 (Free base)
Appearance:
Solid powder
Synonyms:
1'-(4-(1-(4-fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro[isobenzofuran-1,4'-piperidine]; Siramesine free base; Lu-28-179; Lu 28-179; Lu28-179; Lu-28179; Lu 28179; Lu28179
Solubility:
Soluble to ≥ 42 mg/mL in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -86℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
InChIKey:
XWAONOGAGZNUSF-UHFFFAOYSA-N
InChI:
1S/C30H31FN2O/c31-25-12-14-26(15-13-25)33-21-23(27-9-2-4-11-29(27)33)7-5-6-18-32-19-16-30(17-20-32)28-10-3-1-8-24(28)22-34-30/h1-4,8-15,21H,5-7,16-20,22H2
Canonical SMILES:
FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=CC=CC=C45)C6=C2C=CC=C6)C=C1
1.Structural characterisation and dehydration behaviour of siramesine hydrochloride.
Zimmermann A;Tian F;de Diego HL;Frydenvang K;Rantanen J;Elema MR;Hovgaard L J Pharm Sci. 2009 Oct;98(10):3596-607. doi: 10.1002/jps.21679.
In this study the crystal structures of siramesine hydrochloride anhydrate alpha-form and siramesine hydrochloride monohydrate were determined, and this structural information was used to explain the physicochemical properties of the two solid forms. In the crystal structure of the monohydrate, each water molecule is hydrogen bonded to two chloride ions, and thus the water is relatively strongly bound in the crystal. No apparent channels for dehydration were observed in the monohydrate structure, which could allow transmission of structural information during dehydration. Instead destructive dehydration occurred, where the elimination of water from the monohydrate resulted in the formation of an oily phase, which subsequently recrystallised into one or more crystalline forms. Solubility and intrinsic dissolution rate of the anhydrate alpha-form and the monohydrate in aqueous media were investigated and both were found to be lower for the monohydrate compared to the anhydrate alpha-form. Finally, the interactions between water molecules and chloride ions in the monohydrate as well as changes in packing induced by water incorporation could be detected by spectroscopic techniques.
2.Adsorption of pharmaceutical excipients onto microcrystals of siramesine hydrochloride: effects on physicochemical properties.
Zimmermann A;Millqvist-Fureby A;Elema MR;Hansen T;Müllertz A;Hovgaard L Eur J Pharm Biopharm. 2009 Jan;71(1):109-16. doi: 10.1016/j.ejpb.2008.06.014. Epub 2008 Jun 24.
A common challenge in the development of new drug substances is poor dissolution characteristics caused by low aqueous solubility. In this study, microcrystals with optimized physicochemical properties were prepared by precipitation in the presence of excipients, which adsorbed to the particle surface and altered particle size, morphology, and dissolution rate. The poorly water-soluble drug siramesine hydrochloride was precipitated by the antisolvent method in the presence of each of various polymeric and surface active excipients. Powder dissolution studies of six of the resulting particle systems showed a significant increase in percent dissolved after 15 min compared to the starting material. A quantitative determination of the amount of excipient adsorbed to the surface of the drug particles proved that only a very small amount of excipient was needed to exert a marked effect on particle properties. The adsorbed amount of excipient constituted less than 1.4% (w/w) of the total particle weight, and thus powders of very high drug loads were obtained. Sodium lauryl sulphate (SLS), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose (HPC), which exhibited the greatest degree of adsorption, also had the greatest effect on the physicochemical properties of the particles.
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