Miltirone (Synonyms: Rosmariquinone)

Name: Miltirone
Brand: MedChemExpress
SKU: HY-N1951
Rating: 5.0 (2 reviews)

Cat. No.: HY-N1951 Purity: 99.54%: Data Sheet
COA

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Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC₅₀ of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; K_i = 0.04 μM) and SARS-CoV main protease (Mpro).

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

CAS No. : 27210-57-7

Size	Stock	Quantity
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
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Miltirone:

Miltirone (Standard) Get quote

2 Publications Citing Use of MCE Miltirone

Cell Proliferation/Viability Assay

Cell Migration/Invasion Assay

Apoptosis Analysis

ELISA

: Miltirone purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Aug 20;10(16):e36603. [Abstract]; SW620 and HCT116 cells were administrated with 0∼40 μM Miltirone for 0–72 h. MTT assays were performed for cell viability assessment.

: Miltirone purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Aug 20;10(16):e36603. [Abstract]; SW620 and HCT116 cells were treated with 0∼40 μM Miltirone for 72 h. Transwell assays were conducted, migrating and invasive cell number was calculated.

: Miltirone purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Aug 20;10(16):e36603. [Abstract]; Apoptotic cell frequencies treated without or with Miltirone (40 μM) for 24 h were determined by annexin V/PI assays in SW620 and HCT116 cells.

: Miltirone purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Aug 20;10(16):e36603. [Abstract]; IL-1β released into culture medium was detected by ELISA assays treated with Miltirone (40 μM) for 24 h.

: Miltirone purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Aug 20;10(16):e36603. [Abstract]; Release of LDHA proteins to culture mediums were detected by Western blot assays treated with Miltirone (40 μM) for 24 h.

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View All Isoforms

CES1 CES2 CES3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CES2

0.04 μM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	24.59 μM Compound: Miltrone 5	Cytotoxicity against A549 cell line Cytotoxicity against A549 cell line	[PMID: 16434190]
HCT-116	IC₅₀	12.39 μM Compound: Miltrone 5	Cytotoxicity against HCT116 cell line Cytotoxicity against HCT116 cell line	[PMID: 16434190]
Hep 3B2	EC₅₀	14.8 μM Compound: 1	Cytotoxicity against human Hep3B cells after 24 hrs by MTT assay Cytotoxicity against human Hep3B cells after 24 hrs by MTT assay	[PMID: 26339922]
Hep 3B2	EC₅₀	6.6 μM Compound: 1	Cytotoxicity against human Hep3B cells after 24 hrs by MTT assay in presence of doxorubicin Cytotoxicity against human Hep3B cells after 24 hrs by MTT assay in presence of doxorubicin	[PMID: 26339922]
HepG2	EC₅₀	12 μM Compound: 1	Cytotoxicity against human doxorubicin-resistant HepG2 cells expressing p-gp after 24 hrs by MTT assay Cytotoxicity against human doxorubicin-resistant HepG2 cells expressing p-gp after 24 hrs by MTT assay	[PMID: 26339922]
HepG2	EC₅₀	30.9 μM Compound: 1	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay in presence of doxorubicin Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay in presence of doxorubicin	[PMID: 26339922]
HepG2	EC₅₀	7.1 μM Compound: 1	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 26339922]
MIA PaCa-2	IC₅₀	22.5 μM Compound: 17	Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay	[PMID: 21775156]
PLC-PRF-5	EC₅₀	17.4 μM Compound: 1	Cytotoxicity against human PLC/PRF/5 cells after 24 hrs by MTT assay in presence of doxorubicin Cytotoxicity against human PLC/PRF/5 cells after 24 hrs by MTT assay in presence of doxorubicin	[PMID: 26339922]
PLC-PRF-5	EC₅₀	27.1 μM Compound: 1	Cytotoxicity against human PLC/PRF/5 cells after 24 hrs by MTT assay Cytotoxicity against human PLC/PRF/5 cells after 24 hrs by MTT assay	[PMID: 26339922]

In Vitro

Miltirone (0-100 μM, 48 h) induces ROS - and-p53 dependent apoptosis in colon cancer cells^[2].
Miltirone (3.13-25 μM, 1-24 h) induces translocation of apoptosis-inducing factor (AIF) in colon cancer cells^[2].

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

Cell Viability Assay^[2]

Cell Line:	HCT116 p53^+/+, HCT116 p53^-/-, HT29 p53^mut/mut, CCD18-co (normal human colon fibroblast)
Concentration:	0-100 μM
Incubation Time:	48 h
Result:	Showed potent cytotoxicity and pro-apoptotic activity on HCT116 cells. Preferential inhibition of cancer cells was found when comparing its cytotoxicity on colon cancer cells (IC₅₀ = 4.27 μM) with that on normal colon cells (IC₅₀ = 41.3 μM). The pro-apoptotic activity was significantly inhibited by the pretreatment of ROS scavenger or calpeptin. Apoptosis was significantly enhanced when pretreated with Dicoumarol (HY-N0645). In case of p53 deficiency, the apoptosis was obviously decreased.

Western Blot Analysis^[2]

Cell Line:	HCT116
Concentration:	1.56, 3.13, 6.25, 12.5, 25 μM
Incubation Time:	48 h
Result:	Stimulated the activation of caspase-3, -8 and -9 in a concentration-dependent way. Pretreatment of N-acetylcysteine (NAC) (HY-B0215) efficiently inhibited the activation of caspase-3 and caspase-9 but not that of caspase-8.

Western Blot Analysis^[2]

Cell Line:	HCT116
Concentration:	3.13, 6.25, 12.5, 25 μM
Incubation Time:	1, 3, 6, 12, 24 h
Result:	Stimulated time- and concentration-dependent translocation of AIF to cytosol and nuclear. Translocation of AIF to nuclear was partially inhibited by the pretreatment of calpain.

In Vivo

Miltirone (10-60 mg/kg, p.o.; one hour before test) increases the number of punished crossings in the four-plate test in mice^[1].

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

Animal Model:	Mice^[1]
Dosage:	10, 30, 60 mg/kg
Administration:	Oral gavage (p.o.); an hour before test
Result:	Increased the number of punished crossings of mice in the 'Four-Plate Test'. Showed some reversal of the effect of diazepam as expected for a partial agonist. Produced no muscle relaxant effect and did not impair the performance of mice in the Julou-Courvoisier horizontal wire test.

Molecular Weight

282.38

Formula

C₁₉H₂₂O₂

CAS No.

27210-57-7

Appearance

Solid

Color

Orange to red

SMILES

O=C1C(C(C)C)=CC2=C(C3=C(C=C2)C(C)(C)CCC3)C1=O

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (177.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5413 mL	17.7066 mL	35.4133 mL
5 mM	0.7083 mL	3.5413 mL	7.0827 mL
10 mM	0.3541 mL	1.7707 mL	3.5413 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (8.85 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 (8.85 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (249 KB) HNMR (233 KB) RP-HPLC (267 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. C M Lee, et al. Miltirone, a central benzodiazepine receptor partial agonist from a Chinese medicinal herb Salvia miltiorrhiza. Neurosci Lett. 1991 Jun 24;127(2):237-41. [Content Brief]

[2]. Wang L, et al. Miltirone induced mitochondrial dysfunction and ROS-dependent apoptosis in colon cancer cells. Life Sci. 2016 Apr 15;151:224-234. [Content Brief]

[3]. Hatfield MJ, et al. Modulation of esterified drug metabolism by tanshinones from Salvia miltiorrhiza ("Danshen"). J Nat Prod. 2013 Jan 25;76(1):36-44. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.5413 mL	17.7066 mL	35.4133 mL	88.5332 mL
	5 mM	0.7083 mL	3.5413 mL	7.0827 mL	17.7066 mL
	10 mM	0.3541 mL	1.7707 mL	3.5413 mL	8.8533 mL
	15 mM	0.2361 mL	1.1804 mL	2.3609 mL	5.9022 mL
	20 mM	0.1771 mL	0.8853 mL	1.7707 mL	4.4267 mL
	25 mM	0.1417 mL	0.7083 mL	1.4165 mL	3.5413 mL
	30 mM	0.1180 mL	0.5902 mL	1.1804 mL	2.9511 mL
	40 mM	0.0885 mL	0.4427 mL	0.8853 mL	2.2133 mL
	50 mM	0.0708 mL	0.3541 mL	0.7083 mL	1.7707 mL
	60 mM	0.0590 mL	0.2951 mL	0.5902 mL	1.4756 mL
	80 mM	0.0443 mL	0.2213 mL	0.4427 mL	1.1067 mL
	100 mM	0.0354 mL	0.1771 mL	0.3541 mL	0.8853 mL

Miltirone Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Miltirone (Synonyms: Rosmariquinone)

Customer Review

Other Forms of Miltirone:

Miltirone Related Antibodies

2 Publications Citing Use of MCE Miltirone

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Carboxylesterase (CES) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Miltirone Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Miltirone Related Classifications

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