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Heptamidine dimethanesulfonate (Synonyms: SBi4211 dimethanesulfonate)

Cat. No.: HY-16918A
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Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).

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

Heptamidine dimethanesulfonate Chemical Structure

Heptamidine dimethanesulfonate Chemical Structure

CAS No. : 161374-55-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 370 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2].

IC50 & Target

Kd: 6.9 μM (calcium-binding protein S100B)[1]

In Vitro

Heptamidine is a Pentamidine-S100B complex, two molecules of pentamidine bind per monomer of S100B, which performs to be an inhibitor for S100B[1].
Heptamidine (20 μM) does not decrease CUG levels significantly when compares to Propamidine and Pentamidine, and exhibits cytotoxic at concentrations above 17.5 μM in HeLa cells expressing 960 CUG repeats[2].
Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC50 value of 15 μM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) causes a dose-dependent reduction of exon 7a inclusion in HSALR mice, returning to wild type levels (6±1%) when at 20 mg/kg dose, the myotonia is reduced from grade 3 to grade 1 (occasional myotonic discharge) or grade 0 at both 20 or 30 mg/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Homozygous HSALR transgenic mice in line 20b (FVB inbred background) with a Myotonic dystrophy (DM) mouse model[2]
Dosage: 20 or 30 mg/kg
Administration: Intraperitoneal injection; 7 days; once daily
Result: Reversed splicing defects and rescues myotonia in a DM mouse model.
Molecular Weight

560.68

Formula

C₂₃H₃₆N₄O₈S₂

CAS No.

161374-55-6

SMILES

N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.CS(=O)(O)=O.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (111.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7835 mL 8.9177 mL 17.8355 mL
5 mM 0.3567 mL 1.7835 mL 3.5671 mL
10 mM 0.1784 mL 0.8918 mL 1.7835 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: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

HeptamidineSBi4211SBi 4211SBi-4211OthersS100BmelanomacancerMyotonicdystrophyHeLacellDMCalcium-BindingInhibitorinhibitorinhibit

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Heptamidine dimethanesulfonate
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