L-Histidinol dihydrochloride

Name: L-Histidinol dihydrochloride
Brand: MedChemExpress
SKU: HY-W014233
Rating: 4.5 (1 reviews)

Cat. No.: HY-W014233 Purity: ≥98.0%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

L-Histidinol dihydrochloride is an orally active histidyl-tRNA synthetase inhibitor. L-Histidinol dihydrochloride interferes with the initiation stage of protein synthesis, thus affecting cell proliferation and metabolism. L-Histidinol dihydrochloride has the effect of modulating the sensitivity of tumor cells to chemotherapeutic agents. L-Histidinol dihydrochloride reduces the toxicity of certain chemotherapeutic agents to normal tissues and enhance the sensitivity of tumor cells to chemotherapeutic agents.

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

L-Histidinol dihydrochloride Chemical Structure

CAS No. : 1596-64-1

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

L-histidinol (1-15 mM; 4 h pretreatment) dihydrochloride potentiates hyperthermic cell (HeLa and S-180)-killing in-vitro^[1].
L-histidinol (3 mM; 2 h) dihydrochloride inhibits protein and ribosomal RNA synthesis in mouse L cells^[2].
L-histidinol (1-3 mM; 24 h) dihydrochloride shows a modest, dose-dependent toxicity to cultured P815 mastocytoma cells^[3].
L-histidinol (3 mM; 48 h) dihydrochloride, when combined with different anticancer drugs, reverses the multidrug-resistance attribute of CH^RC5 cells^[4].
L-histidinol (1 mM; 24 h) dihydrochloride inhibits the proliferative responses induced by Con A and LPS (HY-D1056) in cultured mouse spleen cells^[5].

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

In Vivo

L-Histidinol (5 mg/injection; i.p.; administered at -2, 0, 2, 4, and 6 h) dihydrochloride, when combined with ara-C (HY-13605) or FUra, eliminates their bone marrow toxicity in DBA/2J mice and enhances the eradication of intraperitoneal P815 mastocytoma cells^[3].
L-Histidinol (250 mg/kg; i.p.) dihydrochloride, in combination with BCNU (HY-13585), improves the treatment effect of P388 leukemia in DBA/2J mice, increasing the median survival time and the number of 60-day survivors^[6].
L-Histidinol dihydrochloride (7 mg/mouse; i.p.; 4 consecutive days a week, with 5 doses at 2-h intervals; for 3 weeks) significantly inhibits tumor growth in CD8F1 breast tumor mice^[7].
L-Histidinol (100 mg/kg; i.p.; once every 2 h for 5 times; starting 2 h before Cisplatin administration) dihydrochloride reduces Cisplatin (HY-17394)-induced nephrotoxicity in rats and protects renal function^[8].
L-Histidinol (0.5%, p.o., drinking water, 3 days before Ifosfamide administration and daily thereafter) dihydrochloride attenuates Fanconi syndrome induced by Ifosfamide (HY-17419) in rats^[9].

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

Animal Model:	Nephrotoxic rats induced by Ifosfamide (HY-17419)^[9]
Dosage:	0.5%
Administration:	Oral gavage (p.o.), drinking water, 3 days before Ifosfamide administration and daily thereafter
Result:	Ameliorated the severity of renal dysfunction. Decreased total and fractional excretions of Na⁺, K⁺, PO₄^3-, and glucose. Decreased serum creatinine and urea levels. Increased the creatinine clearance.

Molecular Weight

214.10

Formula

C₆H₁₃Cl₂N₃O

CAS No.

1596-64-1

Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](CC1=CNC=N1)CO.Cl.Cl

Structure Classification

Others

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (467.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (467.08 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.6708 mL	23.3540 mL	46.7080 mL
5 mM	0.9342 mL	4.6708 mL	9.3416 mL
10 mM	0.4671 mL	2.3354 mL	4.6708 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (11.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (467.08 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (248 KB) HNMR (231 KB)

Handling Instructions (2659 KB)

References

[1]. Kohnoe S, et al. L-histidinol potentiates hyperthermic cell-killing in-vitro. Int J Oncol. 1993 Nov;3(5):835-9. [Content Brief]

[2]. https://pubmed.ncbi.nlm.nih.gov/21573440/ [Content Brief]

[3]. Warrington RC, et al. Effects of L-histidinol on the susceptibility of P815 mastocytoma cells to selected anticancer drugs in vitro and in DBA/2J mice. J Natl Cancer Inst. 1987 Jun;78(6):1177-83. [Content Brief]

[4]. Warrington RC, et al. Reversal of the multidrug-resistant phenotype of Chinese hamster ovary cells by L-histidinol. J Natl Cancer Inst. 1989 May 10;81(10):798-803. doi: 10.1093/jnci/81.10.798. [Content Brief]

[5]. Warrington RC, et al. L-histidinol protection against cytotoxic action of cytosine arabinoside and 5-fluorouracil in cultured mouse spleen cells. J Natl Cancer Inst. 1982 Feb;68(2):279-86. [Content Brief]

[6]. Zaharko D, et al. L-histidinol: preclinical therapeutic studies in combination with antitumor agents and pharmacokinetic studies in mice. Cancer Res. 1992 Jul 1;52(13):3604-9. [Content Brief]

[7]. Stolfi RL, et al. Chemotherapeutic activity of L-histidinol against spontaneous, autochthonous murine breast tumors. Chemotherapy. 1990;36(6):435-40. [Content Brief]

[8]. Badary OA, et al. Effect of L-histidinol on cisplatin nephrotoxicity in the rat. Nephron. 1997;77(4):435-9. [Content Brief]

[9]. Badary OA. L-Histidinol attenuates Fanconi syndrome induced by ifosfamide in rats. Exp Nephrol. 1999 Jul-Aug;7(4):323-7. [Content Brief]

[10]. Warrington RC, et al. L-histidinol improves the selectivity and efficacy of alkylating agents and daunomycin in mice with P388 leukaemia. Br J Cancer. 1989 Nov;60(5):652-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	4.6708 mL	23.3540 mL	46.7080 mL	116.7701 mL
	5 mM	0.9342 mL	4.6708 mL	9.3416 mL	23.3540 mL
	10 mM	0.4671 mL	2.3354 mL	4.6708 mL	11.6770 mL
	15 mM	0.3114 mL	1.5569 mL	3.1139 mL	7.7847 mL
	20 mM	0.2335 mL	1.1677 mL	2.3354 mL	5.8385 mL
	25 mM	0.1868 mL	0.9342 mL	1.8683 mL	4.6708 mL
	30 mM	0.1557 mL	0.7785 mL	1.5569 mL	3.8923 mL
	40 mM	0.1168 mL	0.5839 mL	1.1677 mL	2.9193 mL
	50 mM	0.0934 mL	0.4671 mL	0.9342 mL	2.3354 mL
	60 mM	0.0778 mL	0.3892 mL	0.7785 mL	1.9462 mL
	80 mM	0.0584 mL	0.2919 mL	0.5839 mL	1.4596 mL
	100 mM	0.0467 mL	0.2335 mL	0.4671 mL	1.1677 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.