[CAS NO. 130493-03-7] Bimoclomol
PRODUCTS SPECIFICATIONS [130493-03-7]
DESCRIPTION [130493-03-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 297.78 |
| Molecular Formula | C14H20ClN3O2 |
| SMILES | Cl/C(C1=CC=CN=C1)=N\OCC(O)CN2CCCCC2 |
Summary
Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.
IC50 & Target
|
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 EC 50 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.
Appearance
Oil
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
DMSO : 100 mg/mL ( 335.82 mM ; Need ultrasonic)
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 |
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1.
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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
References
- [1] Jednakovits A, et al. In vivo and in vitro acute cardiovascular effects of bimoclomol. Gen Pharmacol. 2000 May;34(5):363-9.
- [2] Hargitai J, et al. Bimoclomol, a heat shock protein co-inducer, acts by the prolonged activation of heat shock factor-1. Biochem Biophys Res Commun. 2003 Aug 1;307(3):689-95.
- [3] Polakowski JS, et al. Bimoclomol elevates heat shock protein 70 and cytoprotects rat neonatal cardiomyocytes. Eur J Pharmacol. 2002 Jan 18;435(1):73-7.