[CAS NO. 302543-62-0]  Rosiglitazone hydrochloride

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PRODUCTS SPECIFICATIONS [302543-62-0]

Catalog
HY-17386A
Brand
MCE
CAS
302543-62-0

DESCRIPTION [302543-62-0]

Overview

MDL-
Molecular Weight393.89
Molecular FormulaC18H20ClN3O3S
SMILES[H]Cl.O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O

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

83 Publications Citing Use of MCE


Summary

Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist ( EC 50 : 60 nM, K d : 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator ( EC 50 : 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer [1] [2] [4] [7] .


IC50 & Target

PPARγ

40 nM (Kd)

PPARγ

60 nM (EC 50 )

TRPC5

30 μM (EC 50 )

TRPM3


In Vitro

Rosiglitazone hydrochloride (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes [1] .
Rosiglitazone hydrochloride (1 μM, 24 h) activates PPARγ , which binds to NF-α1 promoter to activate gene transcription in neurons [3] .
Rosiglitazone hydrochloride (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner [3] .
Rosiglitazone hydrochloride (0.01-100 μM, 15 min) inhibits TRPM3 with IC 50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively [4] .
Rosiglitazone hydrochloride (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation [7] .
Rosiglitazone hydrochloride (5 μM, 7 days) suppresses Olaparib ( HY-10162 )‑induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells [7] .

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

Cell Proliferation Assay [7]

Cell Line: A2780 and SKOV3 cells
Concentration: 0.5-50 μM
Incubation Time: 1-7 days
Result: Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner.

Western Blot Analysis [3]

Cell Line: Hippocampal neurons
Concentration: 1 μM
Incubation Time: 1 μM
Result: Increased NF-α1 and BCL-2 protein level.

In Vivo

Rosiglitazone hydrochloride (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats [5] .
Rosiglitazone hydrochloride (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats [6] .
Rosiglitazone hydrochloride (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models [7] .

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

Animal Model: Streptozotocin (STZ)-induced diabetic rats [5]
Dosage: 5 mg/kg
Administration: Oral administration, daily for 8 weeks.
Result: Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group.
Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups.
Animal Model: Male Wistar rats [6]
Dosage: 3 mg/kg/day
Administration: Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks
Result: Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS).
Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00636766 Aristotle University Of Thessaloniki
Carotid Atherosclerosis|Stroke|Type 2 Diabetes|Metabolic Syndrome
September 2005 Not Applicable
NCT00143624 University of British Columbia
Atherosclerosis|HIV Infections
June 2003 Not Applicable
NCT00483392 University Medical Centre Ljubljana
Insulin Resistance
Not Applicable

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL ( 158.67 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5388 mL 12.6939 mL 25.3878 mL
5 mM 0.5078 mL 2.5388 mL 5.0776 mL
10 mM 0.2539 mL 1.2694 mL 2.5388 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% Saline

    Solubility: ≥ 10 mg/mL (25.39 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% Corn Oil

    Solubility: 10 mg/mL (25.39 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% Saline

    Solubility: ≥ 10 mg/mL (25.39 mM); Clear solution

* All of the co-solvents are available by MedChemExpress (MCE).