| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
L-Histidinol targets histidyl-tRNA synthetase (HARS), a key enzyme in protein synthesis. It acts as a competitive inhibitor, effectively binding to the active site of the enzyme due to its structural resemblance to histidine. It is also a precursor of histamine and histidine.
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| ln Vitro |
In vitro, L-Histidinol dihydrochloride acts as a potent and reversible inhibitor of protein synthesis in cultured human cells. It inhibits histidyl-tRNA synthetase, blocking the charging of tRNA with histidine and thereby inhibiting protein synthesis initiation. The compound affects cellular proliferation and metabolic processes, making it relevant for cancer research. It serves as a crucial tool in enzyme inhibition studies.
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| ln Vivo |
In vivo, L-Histidinol dihydrochloride is a precursor of histamine and histidine. As a reversible inhibitor of protein synthesis, it may affect cellular proliferation and metabolic processes. The compound's effects on protein synthesis and histidine metabolism suggest potential applications in research on cell growth and metabolism.
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| Enzyme Assay |
In vitro enzyme assays for histidyl-tRNA synthetase involve incubating the enzyme with L-Histidinol dihydrochloride (0.1-100 µM), ATP, and tRNAᴴⁱˢ in Tris-HCl buffer at pH 7.4-8.0, typically at 37°C. The aminoacylation reaction is monitored by measuring the incorporation of radiolabeled histidine into tRNA or by using a pyrophosphate release assay. Inhibition constants are determined from dose-response curves.
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| Cell Assay |
For in vitro cell assays, cells are cultured in medium supplemented with L-Histidinol dihydrochloride at concentrations of 0.1-10 mM. Cell viability and proliferation are assessed by MTT assay. Protein synthesis is measured by monitoring the incorporation of radiolabeled amino acids into proteins or by using puromycin incorporation assays. The compound's effects on cell cycle and apoptosis are evaluated by flow cytometry.
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| Animal Protocol |
For in vivo animal studies, L-Histidinol dihydrochloride is typically administered to rodents via oral gavage or intraperitoneal injection at doses of 10-100 mg/kg. Blood and tissue samples are collected for pharmacokinetic analysis. The compound's effects on protein synthesis are assessed by measuring tissue protein content or by using isotopic labeling techniques. Histidine and histamine levels are quantified by HPLC or LC-MS/MS.
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| ADME/Pharmacokinetics |
L-Histidinol dihydrochloride (MW 214.09) has a melting point of 193-195°C. It is soluble in water and DMSO. The compound is stable under recommended storage conditions (powder at -20°C). As a histidine analog, it is absorbed and metabolized through histidine metabolic pathways. The compound is a reversible inhibitor of protein synthesis and a precursor of histamine.
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| Toxicity/Toxicokinetics |
The compound is for research use only. No specific toxicity data are available. L-Histidinol is a potent inhibitor of protein synthesis and may cause cellular toxicity at high concentrations through inhibition of protein synthesis. Standard safety precautions should be followed when handling.
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| Additional Infomation |
L-histidine dihydrochloride is an aryl amine.
L-Histidinol dihydrochloride (CAS# 1596-64-1) is a research reagent used primarily in studies of protein synthesis, enzyme inhibition, and histidine metabolism. It has not been investigated in clinical trials nor approved as a therapeutic drug. The compound is used in cancer research due to its effects on cellular proliferation and in studies of histidyl-tRNA synthetase function. It is a valuable tool for studying the mechanisms of protein synthesis and amino acid metabolism. |
| Molecular Formula |
C6H13CL2N3O
|
|---|---|
| Molecular Weight |
214.09
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| Exact Mass |
213.043
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| CAS # |
1596-64-1
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| PubChem CID |
197743
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| Appearance |
White to off-white solid powder
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| Boiling Point |
455.5ºC
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| Melting Point |
198-201 °C (dec.)(lit.)
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| Flash Point |
229.3ºC
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| Vapour Pressure |
4.34E-09mmHg at 25°C
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| LogP |
1.576
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
12
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| Complexity |
99
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=C(NC=N1)C[C@@H](CO)N.Cl.Cl
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| InChi Key |
FRCAFNBBXRWXQA-XRIGFGBMSA-N
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| InChi Code |
InChI=1S/C6H11N3O.2ClH/c7-5(3-10)1-6-2-8-4-9-6;;/h2,4-5,10H,1,3,7H2,(H,8,9);2*1H/t5-;;/m0../s1
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| Chemical Name |
(2S)-2-amino-3-(1H-imidazol-5-yl)propan-1-ol;dihydrochloride
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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 |
| 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) |
H2O: 100 mg/mL (467.09 mM)
DMSO: 100 mg/mL (467.09 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.68 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 (11.68 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (467.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6709 mL | 23.3547 mL | 46.7093 mL | |
| 5 mM | 0.9342 mL | 4.6709 mL | 9.3419 mL | |
| 10 mM | 0.4671 mL | 2.3355 mL | 4.6709 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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