[CAS NO. 148717-90-2]  Squalamine

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PRODUCTS SPECIFICATIONS [148717-90-2]

Catalog
HY-16468
Brand
MCE
CAS
148717-90-2

DESCRIPTION [148717-90-2]

Overview

MDL-
Molecular Weight627.96
Molecular FormulaC34H65N3O5S
SMILESC[C@@]12[C@](C[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@@H](CC[C@H](C(C)C)OS(=O)(O)=O)C)([H])C[C@@H](NCCCNCCCCN)CC1

For research use only. We do not sell to patients.

Summary

Squalamine(MSI-1256) is an aminosterol compound with potent broad spectrum antiviral activity. IC50 value: Target: in vitro: squalamine can strongly displace membrane-bound cationic proteins such as Rac1, a ρ-GTPase recruited to the inner leaflet of the eukaryotic cytoplasmic membrane for the actin remodeling necessary for endocytosis. At concentrations between 20 and 60 μg/mL, squalamine has been shown to inhibit a broad array of growth factor-induced, actin-dependent responses in endothelial cells, including cell migration, cell division, and vascular tube formation in a 3D matrix [1]. Squalamine effectively inhibited HBV replication in human primary hepatocytes when added either during the initial exposure of virus to the cells or at 24 h after infection . A similar study was performed to evaluate the effect of squalamine on the replication of HDV. Squalamine was introduced at 20 μg/mL during HDV exposure, and the effects were measured at day 7 when total RNA was extracted and assayed for HDV RNA sequences [1]. in vivo: one time daily treatment with squalamine (15 or 30 mg/kg per d s.c.) was started beginning on day 1 or 2 after viral administration and continuing until day 8 or 9, respectively. Survival was monitored, and animals that remained alive by day 21 were considered cured [1].


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00139282 Genaera Corporation
Wet Age-Related Macular Degeneration
June 2005 Phase 3
NCT02614937 Ohr Pharmaceutical Inc.|Cumberland Valley Retina Consultants, PC
Retinal Vein Occlusion|Macular Edema
April 2013 Phase 1|Phase 2
NCT00333476 Genaera Corporation
Macular Degeneration
May 2006 Phase 2

Appearance

Solid


Source

Squalus acanthias


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 159.25 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5925 mL 7.9623 mL 15.9246 mL
5 mM 0.3185 mL 1.5925 mL 3.1849 mL
10 mM 0.1592 mL 0.7962 mL 1.5925 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Cholestane-7,24-diol, 3-[[3-[(4-aminobutyl)amino]propyl]amino]-, 24-(hydrogen sulfate), (3β,5α,7α,24R)-
Squalamine
MSI 1256