| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Bimoclomol (40 μM) considerably increases coronary flow (CF) during normoxic perfusion (pre-ischemia). Bimoclomol significantly raised LVDP and CO but lowered LVEDP in ischemia circumstances. Bimoclomol displays a biphasic effect on relaxation rate. Bimoclomol (>10 μM) produces concentration-dependent vasodilation with an EC50 value of 214 μM. Bimoclomol (100 μM) similarly causes vasodilation in response to 20 mM KCl. However, bimoclomol is unable to relax agents precontracted with serotonin, PGF2, or angiotensin II [1]. Bimoclomol does not change the stability of Hsp70 or its mRNA. Bimoclomol promotes Hsp expression via delaying the activation of heat shock transcription factor (HSF-1). The effects of bimoclomol were reduced in cells from mice missing HSF-1. In addition, bimoclomol can bind to HSF-1 and cause extended interaction of HSF-1 with homologous DNA sites [2]. Bimoclomol (0.1, 1, and 10 μM) increased cell survival in rat neonatal cardiomyocytes compared with vehicle-treated cells. Bimoclomol (0.01 to 10 μM) significantly elevated HSP70 levels depending on exposure time. Pretreatment with Bimoclomol for 24 hours can considerably boost the survival rate of cells [3].
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| ln Vivo |
In dogs under anesthesia, bimoclomol (1 and 5 mg/kg) can attenuate ST-segment elevation by 56% and 80%, respectively, due to coronary artery blockage [1].
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| References |
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| Additional Infomation |
Bimoclomol is an investigational drug that induces stress proteins and has cytoprotective effects.
Drug Indication Investigated for use/treatment in neuropathy (diabetic) and wounds. Mechanism of Action Bimoclomol binds to HSF-1 and induces a prolonged binding of HSF-1 to the respective DNA elements. Since HSF-1 does not bind to DNA in the absence of stress, the bimoclomol-induced extension of HSF-1/DNA interaction may contribute to the chaperone co-induction of bimoclomol observed previously. These findings indicate that bimoclomol may be of value in targeting HSF-1 so as to induce up-regulation of protective Hsp-s in a non-stressful manner and for therapeutic benefit. |
| Molecular Formula |
C14H20N3O2CL
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|---|---|
| Molecular Weight |
297.7805
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| Exact Mass |
297.124
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| CAS # |
130493-03-7
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| PubChem CID |
9576891
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| Appearance |
Light yellow to brown ointment
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| Density |
1.27g/cm3
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| Boiling Point |
454ºC at 760mmHg
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| Flash Point |
228.4ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
1.783
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
20
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| Complexity |
309
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl/C(C1=CC=CN=C1)=N\OCC(O)CN2CCCCC2
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| InChi Key |
NMOVJBAGBXIKCG-VKAVYKQESA-N
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| InChi Code |
InChI=1S/C14H20ClN3O2/c15-14(12-5-4-6-16-9-12)17-20-11-13(19)10-18-7-2-1-3-8-18/h4-6,9,13,19H,1-3,7-8,10-11H2/b17-14-
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| Chemical Name |
(3Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)pyridine-3-carboximidoyl chloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~335.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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