Troglitazone (Synonyms: CS-045)

Name: Troglitazone
Brand: MedChemExpress
SKU: HY-50935
Rating: 5.0 (24 reviews)

Cat. No.: HY-50935 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

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Troglitazone is an orally active PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.

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

Troglitazone Chemical Structure

CAS No. : 97322-87-7

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Troglitazone:

Troglitazone-d₄ Get quote
Troglitazone (Standard) Get quote

22 Publications Citing Use of MCE Troglitazone

: Troglitazone purchased from MedChemExpress. Usage Cited in: Yonsei Med J. 2018 Nov;59(9):1096-1106. [Abstract]; MCN and N2a cells are treated with Control (DMSO), Troglitazone (Tro; 20 µM), or GW9662 (10 µM) for 24 h, followed by detection of PPAR-γ protein level via Western blot assay.

: Troglitazone purchased from MedChemExpress. Usage Cited in: Breast Cancer Res Treat. 2017 Oct;165(3):517-527. [Abstract]; MDA-MB-231 and Hs578T TNBC ‘‘claudin-1-low’’ cells, and the non-tumorigenic human breast epithelial cell line MCF-10A are treated with 20 μM of TGZ, RGZ, D2-TGZ, or DMSO (Ctrl) for 24 h and subjected to western blot analysis with claudin-1 (CLDN1) antibody. α-tubulin is used as loading control.

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Biological Activity
Protocol
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References
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Description

IC₅₀ & Target^[1]

PPARγ

550 nM (EC₅₀, Human PPARγ)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	15 μM Compound: Troglitazone	Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay	[PMID: 15454234]
CHO	EC₅₀	0.44 μM Compound: troglitazone	Agonist activity at human recombinant PPARgamma expressed in CHO cells cotransfected with pGL3-PPRE3-TK-luc reporter assessed as beta-galactosidase activity at after 24 hrs by luciferase based transactivation assay Agonist activity at human recombinant PPARgamma expressed in CHO cells cotransfected with pGL3-PPRE3-TK-luc reporter assessed as beta-galactosidase activity at after 24 hrs by luciferase based transactivation assay	[PMID: 22424300]
CHO	EC₅₀	0.44 μM Compound: Troglitazone	Agonist activity at human PPARgamma expressed in CHO cells co-transfected with pGL3-PPRE3-TK-luc assessed as transactivation after 24 hrs by firefly luciferase reporter gene assay Agonist activity at human PPARgamma expressed in CHO cells co-transfected with pGL3-PPRE3-TK-luc assessed as transactivation after 24 hrs by firefly luciferase reporter gene assay	[PMID: 22342624]
CV-1	EC₅₀	0.4 μM Compound: Troglitazone	Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 22579420]
HCT-15	IC₅₀	> 100 μM Compound: Tgz	Antitumor activity against human HCT15 cells assessed as inhibition of cell proliferation after 1 day by MTT assay Antitumor activity against human HCT15 cells assessed as inhibition of cell proliferation after 1 day by MTT assay	[PMID: 22081932]
HCT-15	IC₅₀	50.9 μM Compound: Tgz	Antitumor activity against human HCT15 cells assessed as inhibition of cell proliferation after 2 days by MTT assay Antitumor activity against human HCT15 cells assessed as inhibition of cell proliferation after 2 days by MTT assay	[PMID: 22081932]
HEK293	EC₅₀	0.4 μM Compound: Troglitazone	Activation of PPARgamma transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control Activation of PPARgamma transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control	[PMID: 21800856]
HEK-293T	IC₅₀	4.5 μM Compound: Troglitazone	Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis	[PMID: 23122865]
HEK-293T	IC₅₀	61 μM Compound: Troglitazone	Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis	[PMID: 23122865]
HepG2	EC₅₀	0.72 μM Compound: TGZ	Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay	[PMID: 23031596]
HepG2	EC₅₀	0.73 μM Compound: Troglitazone	Transactivation of GAL4-fused PPARgamma LBD expressed in HepG2 cells after 20 hrs by luminescence assay Transactivation of GAL4-fused PPARgamma LBD expressed in HepG2 cells after 20 hrs by luminescence assay	[PMID: 22381047]
HepG2	EC₅₀	31.6 μM Compound: Troglitazone	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	6.9 μM Compound: Troglitazone	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
Hs-578T	IC₅₀	> 100 μM Compound: TGZ	Antiproliferative activity against human Hs578T cells in 10% FCS by crystal violet staining based assay Antiproliferative activity against human Hs578T cells in 10% FCS by crystal violet staining based assay	[PMID: 31838327]
HT-29	IC₅₀	> 100 μM Compound: Tgz	Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation after 1 day by MTT assay Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation after 1 day by MTT assay	[PMID: 22081932]
HT-29	IC₅₀	50 μM Compound: Tgz	Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation after 2 days by MTT assay Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation after 2 days by MTT assay	[PMID: 22081932]
LNCaP	IC₅₀	22 μM Compound: Troglitazone	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay	[PMID: 22546208]
LoVo	IC₅₀	> 100 μM Compound: Tgz	Antitumor activity against human LoVo cells assessed as inhibition of cell proliferation after 1 day by MTT assay Antitumor activity against human LoVo cells assessed as inhibition of cell proliferation after 1 day by MTT assay	[PMID: 22081932]
LoVo	IC₅₀	65 μM Compound: Tgz	Antitumor activity against human LoVo cells assessed as inhibition of cell proliferation after 2 days by MTT assay Antitumor activity against human LoVo cells assessed as inhibition of cell proliferation after 2 days by MTT assay	[PMID: 22081932]
MCF7	IC₅₀	35.4 μM Compound: TGZ	Antiproliferative activity hormone-dependent human MCF7 cells after 24 hrs by luminescent cell viability assay Antiproliferative activity hormone-dependent human MCF7 cells after 24 hrs by luminescent cell viability assay	[PMID: 22409968]
MCF7	IC₅₀	74.3 μM Compound: TGZ	Antiproliferative activity against human MCF7 cells in 10% FCS by crystal violet staining based assay Antiproliferative activity against human MCF7 cells in 10% FCS by crystal violet staining based assay	[PMID: 31838327]
MDA-MB-231	IC₅₀	15.7 μM Compound: TGZ	Antiproliferative activity hormone-independent human MDA-MB-231 cells after 24 hrs by luminescent cell viability assay Antiproliferative activity hormone-independent human MDA-MB-231 cells after 24 hrs by luminescent cell viability assay	[PMID: 22409968]
MDA-MB-231	IC₅₀	45.5 μM Compound: TGZ	Antiproliferative activity against human MDA-MB-231 cells in 10% FCS by crystal violet staining based assay Antiproliferative activity against human MDA-MB-231 cells in 10% FCS by crystal violet staining based assay	[PMID: 31838327]
MDA-MB-453	IC₅₀	67.1 μM Compound: TGZ	Antiproliferative activity against human MDA-MB-453 cells in 10% FCS by crystal violet staining based assay Antiproliferative activity against human MDA-MB-453 cells in 10% FCS by crystal violet staining based assay	[PMID: 31838327]
Mesenchymal stem cells	EC₅₀	0.1 μM Compound: Tro	Induction of adiponectin synthesis in human differentiated BMMSC cells measured after 5 days in the presence of IDX induction medium by ELISA Induction of adiponectin synthesis in human differentiated BMMSC cells measured after 5 days in the presence of IDX induction medium by ELISA	[PMID: 34922307]
PC-12	IC₅₀	15 μM Compound: 1a, Tro	Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay	[PMID: 15109648]
PC-3	IC₅₀	30 μM Compound: Troglitazone	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	[PMID: 22546208]
Ventricular myocyte	IC₅₀	9.5 μM Compound: Troglitazone	Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes	[PMID: 22761000]

In Vitro

Troglitazone (2-200 μM, 24 h) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC₅₀s of 49.9±1.2 and 51.3±5.3 μM, respectively^[2].
Troglitazone (50 μM, 24 h) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression^[2].
Troglitazone (0-4 μM, 12 h) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells (A549, HCC-15 and Calu-3)^[3].
Troglitazone (0-4 μM, 12 h) induces autophagy and sensitized apoptosis mediated by TRAIL in A549 cells^[1].

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

In Vivo

Troglitazone (200 mg/kg, p.o., every day for 5 weeks) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model^[2].

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

Clinical Trial

Molecular Weight

441.54

Formula

C₂₄H₂₇NO₅S

CAS No.

97322-87-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(SC1CC(C=C2)=CC=C2OCC3(C)OC(C(CC3)=C4C)=C(C)C(C)=C4O)NC1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (283.10 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	2.2648 mL	11.3240 mL	22.6480 mL
5 mM	0.4530 mL	2.2648 mL	4.5296 mL
10 mM	0.2265 mL	1.1324 mL	2.2648 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 (5.66 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: ≥ 2.08 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (22.65 mM); Suspended 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: 99.78%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50. [Content Brief]

[2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91. [Content Brief]

[3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831. [Content Brief]

[4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6. [Content Brief]

Cell Assay ^[2]	Briefly, cells are seeded into 96-well plates at a density of 1 × 10⁵ cells/well and incubated for 24 h. The cells are treated with Troglitazone in the presence or absence of other chemicals for a further 24 h using FBS-free medium. The assay utilizes the conversion of alamar blue reagent to fluorescent resorufin by metabolically active cells. The resorufin signal is measured at an excitation wavelength of 530 nm and an emission wavelength of 580 nm. The 50% growth inhibitory concentrations (IC₅₀) are calculated according to the sigmoid inhibitory effect model E = IC₅₀ γ/(IC₅₀ γ + Cγ), where E represents the surviving fraction (% of control), C represents the drug concentration in the medium, and γ represents the Hill coefficient. For co-exposure studies, the Troglitazone dosage is set to approximately the IC₅₀ value for each cell line^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Balb/c male mice (4 weeks old) are subcutaneously inoculated in the back with MIA Paca2 cells (5 × 10⁶ cells/100 μL in PBS) 14 days prior to starting Troglitazone administration. Mice are then orally administered 200 mg/kg Troglitazone in 0.5% methylcellulose solution or vehicle daily for 5 weeks. Tumor size is measured bi-dimensionally and the volume is calculated using the formula (length × width²) × 0.5. Body weights of mice are also monitored throughout the experiment^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50. [Content Brief] [2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91. [Content Brief] [3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831. [Content Brief] [4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2648 mL	11.3240 mL	22.6480 mL	56.6200 mL
	5 mM	0.4530 mL	2.2648 mL	4.5296 mL	11.3240 mL
	10 mM	0.2265 mL	1.1324 mL	2.2648 mL	5.6620 mL
	15 mM	0.1510 mL	0.7549 mL	1.5099 mL	3.7747 mL
	20 mM	0.1132 mL	0.5662 mL	1.1324 mL	2.8310 mL
	25 mM	0.0906 mL	0.4530 mL	0.9059 mL	2.2648 mL
	30 mM	0.0755 mL	0.3775 mL	0.7549 mL	1.8873 mL
	40 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4155 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1324 mL
	60 mM	0.0377 mL	0.1887 mL	0.3775 mL	0.9437 mL
	80 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
	100 mM	0.0226 mL	0.1132 mL	0.2265 mL	0.5662 mL

Troglitazone 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.

Keywords:

Troglitazone97322-87-7CS-045CS045CS 045PPARAutophagyApoptosisFerroptosisPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Troglitazone (Synonyms: CS-045)

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Troglitazone Related Antibodies

22 Publications Citing Use of MCE Troglitazone

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References

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