Daurisoline (Synonyms: (R,R)-Daurisoline)

Name: Daurisoline
Brand: MedChemExpress
SKU: HY-N0221
Rating: 5.0 (2 reviews)

Cat. No.: HY-N0221 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer.

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

Daurisoline Chemical Structure

CAS No. : 70553-76-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 113	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 113	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 324	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 564	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 2 publication(s) in Google Scholar

Other Forms of Daurisoline:

Daurisoline-d₂ Get quote
Daurisoline-d₅ Get quote
Daurisoline-d₁₁ Get quote

2 Publications Citing Use of MCE Daurisoline

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

hERG^[1], autophagy^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
A673	GI₅₀	9.2 μM Compound: 17	Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human A673 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
HCC1806	GI₅₀	17 μM Compound: 17	Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human HCC1806 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
HCC1937	GI₅₀	6.9 μM Compound: 17	Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human HCC1937 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
HCC70	GI₅₀	8.8 μM Compound: 17	Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human HCC70 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
HEK293	IC₅₀	9.1 μM Compound: 1	Inhibition of human ERG stepped current expressed in HEK293 cells at + 20 mV holding potential by patch clamp assay Inhibition of human ERG stepped current expressed in HEK293 cells at + 20 mV holding potential by patch clamp assay	[PMID: 22974355]
HEK293	IC₅₀	9.6 μM Compound: 1	Inhibition of human ERG tail current expressed in HEK293 cells at + 60 mV holding potential by patch clamp assay Inhibition of human ERG tail current expressed in HEK293 cells at + 60 mV holding potential by patch clamp assay	[PMID: 22974355]
MDA-MB-231	GI₅₀	13 μM Compound: 17	Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
MDA-MB-453	GI₅₀	9 μM Compound: 17	Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-453 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]
SJRH30	GI₅₀	3.7 μM Compound: 17	Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay Antiproliferative activity against human SJRH30 assessed as cell growth inhibition after 48 hrs by SRB assay	[PMID: 33226219]

In Vitro

Daurisoline (compound 1) shows a maximal inhibitory effect on the end of depolarization (I_hERG-step) at +20 mV and on the peak tail current (I_hERG-tail) at +60 mV. At concentrations of 1, 3, 10, and 30 μM, the inhibition ratios for current amplitude at the end of depolarization (I_hERG-step) are 32.2±4.2%, 41.6±2.6%, 62.1±5.9%, and 74.8±6.8%, respectively; the IC₅₀ is 9.1 μM. In turn, the inhibition ratios for I_hERG-tail are 16.7±5.8%, 31.1±4.5%, 55.1±7.2%, and 81.2±7.0%, respectively; the IC₅₀ is 9.6 μM^[1]. Daurisoline (DAS) inhibits the CPT-induced autophagy in different cancer cell lines, with IC₅₀s of 74.75±1.03, 50.54±1.02 and 80.81±1.10 μM in HeLa, A549 and HCT-116 cells, respectively. DAC and Daurisoline also impair lysosomal function and lysosomal acidification, via inhibiting the lysosome V-type ATPase acitivity in DAC and Daurisoline treated cells^[2].

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

In Vivo

The results show that plasma concentration exists a biexponential decline following iv administration of Daurisoline (DS) or dauricine (Dau) 6 mg/kg. After iv Daurisoline and Dau 6 mg/kg in beagle dogs, HR, LVSP, dp/dtmax, and SBP are decreased. But the maximum pharmacological effects of both drugs peak at 10 to15 min later than the maximum plasma concentration is observed^[3].

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

Molecular Weight

610.74

Formula

C₃₇H₄₂N₂O₆

CAS No.

70553-76-3

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC2=C(C=C1OC)CCN(C)[C@@H]2CC3=CC=C(O)C(OC4=CC=C(C[C@H]5N(C)CCC6=C5C=C(OC)C(OC)=C6)C=C4)=C3

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (163.74 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	1.6374 mL	8.1868 mL	16.3736 mL
5 mM	0.3275 mL	1.6374 mL	3.2747 mL
10 mM	0.1637 mL	0.8187 mL	1.6374 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (4.09 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 (4.09 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 (4.09 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: 50% PEG300 50% Saline
Solubility: 20 mg/mL (32.75 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.

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).

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: 99.67%

Select Batch:

Data Sheet (279 KB) SDS (392 KB)

COA (248 KB) LCMS (86 KB)

Handling Instructions (2659 KB)

References

[1]. Liu Q, et al. Effect of daurisoline on HERG channel electrophysiological function and protein expression. J Nat Prod. 2012 Sep 28;75(9):1539-45. [Content Brief]

[2]. Wu MY, et al. Natural autophagy blockers, dauricine (DAC) and daurisoline (DAS), sensitize cancer cells tocamptothecin-induced toxicity. Oncotarget. 2017 Sep 8;8(44):77673-77684. [Content Brief]

[3]. Shi SJ, et al. Pharmacokinetic-pharmacodynamic modeling of daurisoline and dauricine in beagle dogs. Acta Pharmacol Sin. 2003 Oct;24(10):1011-5. [Content Brief]

Kinase Assay ^[2]	HEK293 cells are incubated overnight with 35 μg/mL Dx-OG514. Cells are washed and incubated with serum-free Dulbecco's modified Eagle's medium (DMEM) for 2 h. 15 minutes prior to lysis, FCCP is added into the medium to a final concentration of 1 μM. Cells are scraped in fraction buffer (50 mM KCl, 90 mM K-Gluconate, 1 mM EGTA, 50 mM Glucose, 20 mM HEPES, protease inhibitor cocktail, pH=7.4) supplemented with 1 μM FCCP. After spraying with needle, cells are spun down at 10,000 rpm for 15 sec. at 4°C. Then, re-centrifuge the supernatant at max speed for another 20 minutes. The pellet is resuspended in pre-warmed fractionation buffer supplemented with 1% BSA, and split into several aliquots with DAC, Daurisoline (DAS) or BAF treatment for 30 min. Baseline fluorescence is measured at 530 nm upon 511 nm excitation in 96-well plate at 30 s intervals for 5 min^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	Cell proliferation is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. HeLa cells are seeded at 7000 cells per well in 96-well plates in DMEM (1% serum). After cells are treated with different compounds (including Daurisoline) for indicated times, 20 μL of MTT (2.5 mg/mL in PBS) is added to each well. The plates are incubated for an additional 4 h at 37°C. Then the purple-blue MTT formazan precipitate is dissolved in 100 μL DMSO. The cell viability of HeLa cell is evaluated by measuring optical density at 572 nm with a microplate reader^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	After the beagle dogs are anesthetized with sodium pentobarbital (30 mg/kg, iv) a canula is advanced into the left ventricle through the right common carotid artery. And the canula is connected to a pressure transducer which is connected to an amplifier and polygraph. The right femoral artery is canulated to measure the blood pressure wave. ECG (lead II) is observed simultaneously. After iv injection of Daurisoline (DS) (n=4) or Dau (n=4) to beagle dogs, the ECG, BP, and LVP signals are recorded. Blood samples are taken before dosing and at 2, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 6, 8 h after dosing^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Liu Q, et al. Effect of daurisoline on HERG channel electrophysiological function and protein expression. J Nat Prod. 2012 Sep 28;75(9):1539-45. [Content Brief] [2]. Wu MY, et al. Natural autophagy blockers, dauricine (DAC) and daurisoline (DAS), sensitize cancer cells tocamptothecin-induced toxicity. Oncotarget. 2017 Sep 8;8(44):77673-77684. [Content Brief] [3]. Shi SJ, et al. Pharmacokinetic-pharmacodynamic modeling of daurisoline and dauricine in beagle dogs. Acta Pharmacol Sin. 2003 Oct;24(10):1011-5. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.6374 mL	8.1868 mL	16.3736 mL	40.9339 mL
	5 mM	0.3275 mL	1.6374 mL	3.2747 mL	8.1868 mL
	10 mM	0.1637 mL	0.8187 mL	1.6374 mL	4.0934 mL
	15 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7289 mL
	20 mM	0.0819 mL	0.4093 mL	0.8187 mL	2.0467 mL
	25 mM	0.0655 mL	0.3275 mL	0.6549 mL	1.6374 mL
	30 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3645 mL
	40 mM	0.0409 mL	0.2047 mL	0.4093 mL	1.0233 mL
	50 mM	0.0327 mL	0.1637 mL	0.3275 mL	0.8187 mL
	60 mM	0.0273 mL	0.1364 mL	0.2729 mL	0.6822 mL
	80 mM	0.0205 mL	0.1023 mL	0.2047 mL	0.5117 mL
	100 mM	0.0164 mL	0.0819 mL	0.1637 mL	0.4093 mL

Daurisoline 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.

Keywords:

Daurisoline70553-76-3(R,R)-DaurisolineAutophagyPotassium ChannelKcsAantiarrhythmicalkaloidMenispermum dauricumRhizoma MenispermiInhibitorinhibitorinhibit

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Daurisoline (Synonyms: (R,R)-Daurisoline)

Customer Review

Other Forms of Daurisoline:

Daurisoline Related Antibodies

2 Publications Citing Use of MCE Daurisoline

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•Related Screening Libraries:

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Protocol

Purity & Documentation

References

Customer Review

Daurisoline Related Antibodies

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Complete Stock Solution Preparation Table

Daurisoline Related Classifications

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