Lupeol (Synonyms: Clerodol; Monogynol B; Fagarasterol)

Name: Lupeol
Brand: MedChemExpress
SKU: HY-N0790
Rating: 5.0 (3 reviews)

Cat. No.: HY-N0790 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).

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

Lupeol Chemical Structure

CAS No. : 545-47-1

Size	Stock	Quantity
Solution
10 mM * 1 mL in Ethanol	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Lupeol (Standard) Get quote

3 Publications Citing Use of MCE Lupeol

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Description

IC₅₀ & Target

Androgen receptor^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	> 10 μM Compound: 21	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	[PMID: 24467317]
A549	IC₅₀	> 10 μM Compound: 21	Cytotoxicity against human A549 cells after 96 hrs by MTT assay Cytotoxicity against human A549 cells after 96 hrs by MTT assay	[PMID: 24467317]
A549	IC₅₀	> 20 μg/mL Compound: Lupeol	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 21106454]
A549	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human A549 cells by resazurin reduction test Cytotoxicity against human A549 cells by resazurin reduction test	[PMID: 19285391]
A549	IC₅₀	25.18 μM Compound: Lupeol	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31784199]
B16	IC₅₀	38 μM Compound: 1	Growth inhibition of mouse B16 2F2 cells after 3 days Growth inhibition of mouse B16 2F2 cells after 3 days	[PMID: 12027734]
B16	ED₅₀	9.9 μM Compound: 1	Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days	[PMID: 12027734]
Bel-7402	IC₅₀	> 10 μM Compound: 21	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay	[PMID: 24467317]
BGC-823	IC₅₀	> 10 μM Compound: 21	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay	[PMID: 24467317]
BHY	IC₅₀	25.18 μM Compound: Lupeol	Antiproliferative activity against human BHY cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human BHY cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31784199]
BV-2	IC₅₀	> 10 μM Compound: 21	Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method	[PMID: 24467317]
BV-2	IC₅₀	> 100 μM Compound: 35	Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs in presence of LPS by Griess reaction based assay	[PMID: 28911817]
Ca9-22	IC₅₀	16.78 μg/mL Compound: Lupeol	Cytotoxicity against human Ca9-22 cells by MTT assay Cytotoxicity against human Ca9-22 cells by MTT assay	[PMID: 21106454]
Calu-1	IC₅₀	> 100 μM Compound: 5	Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of human Calu1 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]
COLO 205	IC₅₀	25.18 μM Compound: Lupeol	Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31784199]
DLD-1	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human DLD1 cells by resazurin reduction test Cytotoxicity against human DLD1 cells by resazurin reduction test	[PMID: 19285391]
HCT-8	IC₅₀	> 10 μM Compound: 21	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	[PMID: 24467317]
HeLa	IC₅₀	> 10 μg/mL Compound: lupeol	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity against human HeLa cells after 48 hrs by MTT assay	[PMID: 16038541]
HeLa	IC₅₀	> 100 μM Compound: 5	Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of human HeLa cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]
HeLa	IC₅₀	> 50 μM Compound: 5	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 19447618]
Hep 3B2	IC₅₀	18.83 μg/mL Compound: Lupeol	Cytotoxicity against human Hep3B cells by MTT assay Cytotoxicity against human Hep3B cells by MTT assay	[PMID: 21106454]
HEp-2	IC₅₀	> 10 μg/mL Compound: lupeol	Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay	[PMID: 16038541]
HepG2	IC₅₀	19.78 μg/mL Compound: Lupeol	Cytotoxicity against human HepG2 cells by MTT assay Cytotoxicity against human HepG2 cells by MTT assay	[PMID: 21106454]
J774	IC₅₀	> 234.3 μM Compound: 3	Cytotoxicity against mouse J774 cells by alamar blue assay Cytotoxicity against mouse J774 cells by alamar blue assay	[PMID: 17637068]
J774.A1	IC₅₀	34.5 μM Compound: 1, Lupeol	Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method	[PMID: 24909081]
K562	IC₅₀	> 100 μM Compound: 5	Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of human K562 cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]
K562	IC₅₀	82.8 μg/mL Compound: Lupeol	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 32527555]
MCF7	IC₅₀	> 20 μg/mL Compound: Lupeol	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 21106454]
MCF7	IC₅₀	> 50 μM Compound: 5	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 19447618]
MCF7	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human MCF7 cells by resazurin reduction test Cytotoxicity against human MCF7 cells by resazurin reduction test	[PMID: 19285391]
MCF7	IC₅₀	25.18 μM Compound: Lupeol	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31784199]
MDA-MB-231	IC₅₀	> 20 μg/mL Compound: Lupeol	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	[PMID: 21106454]
MIA PaCa-2	IC₅₀	25.18 μM Compound: Lupeol	Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31784199]
Neutrophil	IC₅₀	11.35 μg/mL Compound: 1	Immunomodulatory activity in neutrophils assessed as decrease in oxidative burst after 30 min by luminol-enhanced chemiluminescence assay Immunomodulatory activity in neutrophils assessed as decrease in oxidative burst after 30 min by luminol-enhanced chemiluminescence assay	10.1007/s00044-012-0183-y
PBL	IC₅₀	13.16 μg/mL Compound: 1	Antiproliferative activity against PHA-induced Homo sapiens (human) peripheral blood lymphocytes assessed as inhibition of [3H]-thymidine incorporation after 72 hr by beta-scintillation counting analysis Antiproliferative activity against PHA-induced Homo sapiens (human) peripheral blood lymphocytes assessed as inhibition of [3H]-thymidine incorporation after 72 hr by beta-scintillation counting analysis	10.1007/s00044-012-0183-y
PC-3	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human PC3 cells by resazurin reduction test Cytotoxicity against human PC3 cells by resazurin reduction test	[PMID: 19285391]
Raji	IC₅₀	> 100 μM Compound: 5	Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of human Raji cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]
RAW264.7	IC₅₀	> 0.4 μM Compound: 20(29)-lupen-3-ol	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs	[PMID: 20192236]
RAW264.7	IC₅₀	37.3 μM Compound: 1, Lupeol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method	[PMID: 24909081]
SK-MEL-1	IC₅₀	> 50 μM Compound: 5	Cytotoxicity against human SK-MEL-1 cells by MTT assay Cytotoxicity against human SK-MEL-1 cells by MTT assay	[PMID: 19447618]
Vero	IC₅₀	> 10 μg/mL Compound: lupeol	Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay	[PMID: 16038541]
Vero	IC₅₀	> 100 μM Compound: 5	Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of african green monkey Vero cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]
WISH	IC₅₀	> 100 μM Compound: 5	Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting Inhibition of human WISH cell proliferation assessed as [3H]thymidine incorporation after 3 days by scintillation counting	[PMID: 11374975]

In Vitro

Lupeol, an effective AR inhibitor, can be developed as a potential agent to treat human prostate cancer (CaP). Lupeol (10–50 μM) treatment for 48 h results in a dose-dependent growth inhibition of androgen-dependent phenotype (ADPC) cells viz., LAPC4 and LNCaP cells with an IC₅₀ of 15.9 and 17.3 μM, respectively. Lupeol also inhibits the growth of 22Rν_1 with an IC₅₀ of 19.1 μM. Further, Lupeol inhibits the growth of C4-2b cells with an IC₅₀ of 25 μM. Lupeol has the potential to inhibit the growth of CaP cells of both ADPC and CRPC phenotype. Androgens by activating AR are known to drive the growth of CaP cells^[1].

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

In Vivo

Lupeol is an effective agent that has the potential to inhibit the tumorigenicity of CaP cells in vivo. At the conclusion of the study on day 56, the total circulating serum-PSA levels (secreted by the implanted tumor cells) are measured. At 56thday post-implantation, PSA levels are observed between 11.95-12.79 ng/mL in control animals with LNCaP-tumors and C4-2b-tumors, respectively. However, Lupeol-treated counterpart animals exhibits reduced serum-PSA levels in a range of 4.25-7.09 ng/mL. Tumor tissues of animals receiving Lupeol treatment exhibits reduced serum-PSA levels as compared to control^[1].

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

Clinical Trial

Molecular Weight

426.72

Formula

C₃₀H₅₀O

CAS No.

545-47-1

Appearance

Solid

Color

White to off-white

SMILES

C[C@]1([C@@]2(CC[C@@]3([H])C4(C)C)C)[C@@](CC[C@]2([H])[C@]3(CC[C@@H]4O)C)([H])[C@]([C@@H]5C(C)=C)([H])[C@](C)(CC5)CC1

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:

Ethanol : 14.29 mg/mL (33.49 mM; ultrasonic and warming and heat to 60°C)

DMSO : 2 mg/mL (4.69 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	2.3435 mL	11.7173 mL	23.4346 mL
5 mM	0.4687 mL	2.3435 mL	4.6869 mL
10 mM	0.2343 mL	1.1717 mL	2.3435 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% EtOH 90% Corn Oil
Solubility: ≥ 1.43 mg/mL (3.35 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 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 EtOH stock solution (14.3 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: Corn Oil
Solubility: 20 mg/mL (46.87 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: ≥98.0%

Select Batch:

Data Sheet (282 KB) SDS (392 KB)

COA (254 KB) HNMR (257 KB)

Handling Instructions (2659 KB)

References

[1]. Siddique HR, et al. Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy. Clin Cancer Res. 2011 Aug 15;17(16):5379-91. [Content Brief]

Cell Assay ^[1]	LAPC4 (wild-functional AR/ADPC); LNCaP (mutant-functional AR/ADPC); 22Rν1 (mutant-functional AR/androgen-independent but responsive); C4-2b cells (mutant-functional AR/CRPC) and PC-3 and DU-145 (lack of endogenous AR) are grown under standard cell culture conditions at 37°C and 5% CO₂ environment. The cells (60-70% confluent) are treated with Lupeol (10-50 μM) for 48 h in complete growth medium. For combination set of experiments, cells are treated with either agonistic androgen-analogue R1881 (1 nM), or antagonist Bicalutamide (10 μM), and/or combination (R1881+Lupeol) for 48 h. After incubation for specified times at 37°C, MTT assay is performed. For sensitization studies, hormone refractory C4-2b cells are treated with Lupeol for 24 h. After 24 h, cells are incubated with Bicalutamide (10 μM) for further 24 h. Cells are assessed for viability^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Tumor studies are conducted in athymic nude mice and two cohorts of animals are created. 3×10⁶ of cells are injected subcutaneously in the right flanks of each mouse. Each cohort receive a specific cell type either LNCaP or C4-2b. One week post-implantation, twenty mice (with visible tumors) in each cohort are randomly divided into two groups, with 10 animals in each group. The first group of animals receive intraperitoneal (i.p.) administration of corn oil (100 μL) and served as control. The second group of animals receive i.p. administration of Lupeol (40 mg/kg in 100 μL of corn oil) three times/week. Body weights and tumor volumes are recorded. All animals of group 1 and group 2 are sacrificed when tumors cross a pre-set endpoint volume of 1,000 mm³. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Siddique HR, et al. Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy. Clin Cancer Res. 2011 Aug 15;17(16):5379-91. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / Ethanol	1 mM	2.3435 mL	11.7173 mL	23.4346 mL	58.5864 mL
Ethanol	5 mM	0.4687 mL	2.3435 mL	4.6869 mL	11.7173 mL
	10 mM	0.2343 mL	1.1717 mL	2.3435 mL	5.8586 mL
	15 mM	0.1562 mL	0.7812 mL	1.5623 mL	3.9058 mL
	20 mM	0.1172 mL	0.5859 mL	1.1717 mL	2.9293 mL
	25 mM	0.0937 mL	0.4687 mL	0.9374 mL	2.3435 mL
	30 mM	0.0781 mL	0.3906 mL	0.7812 mL	1.9529 mL

Lupeol Related Classifications

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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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Lupeol (Synonyms: Clerodol; Monogynol B; Fagarasterol)

Customer Review

Other Forms of Lupeol:

3 Publications Citing Use of MCE Lupeol

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•Related Screening Libraries:

•Related Small Molecules:

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Biological Activity

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Purity & Documentation

References

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Complete Stock Solution Preparation Table

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Lupeol (Synonyms: Clerodol; Monogynol B; Fagarasterol)

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Other Forms of Lupeol:

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3 Publications Citing Use of MCE Lupeol

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Purity & Documentation

References

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Complete Stock Solution Preparation Table

Lupeol Related Classifications

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