1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. Bimoclomol

Bimoclomol 

Cat. No.: HY-U00398 Purity: 99.19%
Handling Instructions

Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.

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

Bimoclomol Chemical Structure

Bimoclomol Chemical Structure

CAS No. : 130493-03-7

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5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2400 In-stock
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100 mg USD 3600 In-stock
Estimated Time of Arrival: December 31
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Description

Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.

IC50 & Target[1]

HSP

 

In Vitro

Bimoclomol (40 μM) significantly increases coronary flow (CF) in the period of normoxic perfusion (before ischemia). Bimoclomol significantly increases LVDP and CO, but it decreases LVEDP under ischemic conditions. Bimoclomol displays a biphasic effect on the rate of relaxation. Bimoclomol (>10 μM) causes concentration-dependent vasorelaxation, with EC50 value of 214 μM. Bimoclomol (100 μM) induces vasorelaxation also against 20 mM KCl. However, bimoclomol fails to relax preparations precontracted with serotonin, PGF2 or angiotensin II[1]. Bimoclomol does not affect the stability of Hsp70 or its mRNA. Bimoclomol coinduces Hsp expression via the prolonged activation of the heat shock transcription factor (HSF-1). The effects of bimoclomol are abolished in cells from mice lacking HSF-1. Furthermore, bimoclomol can bind to HSF-1 and induce a prolonged binding of HSF-1 to the respective DNA elements[2]. Bimoclomol (0.1, 1 and 10 μM) improves cell survival of rat neonatal cardiomyocytes compared to vehicle-treated cells. Bimoclomol (0.01 to 10 μM) significantly elevates HSP70 levels, based on the time of exposure. Pretreatment with bimoclomol for 24 h significantly increases survival of cells[3].

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

In Vivo

Bimoclomol (1 and 5 mg/kg) decreases the ST-segment elevation induced by coronary occlusion by 56% and 80%, respectively, in anesthetized dogs[1].

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

Molecular Weight

297.78

Formula

C14H20ClN3O2

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (335.82 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3582 mL 16.7909 mL 33.5818 mL
5 mM 0.6716 mL 3.3582 mL 6.7164 mL
10 mM 0.3358 mL 1.6791 mL 3.3582 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: ≥ 2.5 mg/mL (8.40 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.40 mM); Clear solution

*All of the co-solvents are available by MCE.
References
Cell Assay
[3]

Using the same cell preparation, a cytoprotection (cell survival) assay is configured to assess the ability of bimoclomol to protect cells exposed to a lethal stress. To optimize the cell survival determinations, final plating densities for this protocol are reduced to approximately 0.5 million cells/mL. Plated cardiomyocytes are placed in an incubator (37°C, 5% CO2) for 24 h. The plates are removed from the incubator and the media changed to serum free. Separate sets of cells are either heat shocked at 42°C for 1 h or treated as sham (no heat shock). Bimoclomol is then added to individual wells at 0, 0.01, 0.1, 1, 10 and 100 μM and the plates are placed back in the 37°C incubator for 24 h. The plates are removed from the incubator and after another media change, (serum free) all plates are exposed to a lethal heat stress for 2 h in a waterbath set at 47°C. The plates are then placed back in the 37°C incubator overnight (16-18 h). The following morning, cell survival is determined using trypan blue exclusion. Equal volumes of culture medium and trypan blue solution are mixed. After removing the spent media from the wells, the above mixture is added to the wells for 10 min. The cells are then washed three times with cold PBS and counted with an inverted light microscope (10×). The final survival values from this protocol are expressed as the percentage of viable cells per treatment using the formula [(stained cells−total cells)÷total cells]×100.

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

References
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