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Netoglitazone  (Synonyms: MCC-555; Isaglitazone)

Cat. No.: HY-100428 Purity: 99.92%
Handling Instructions Technical Support

Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus.

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Netoglitazone

Netoglitazone 화학구조

CAS No. : 161600-01-7

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus[1][2][3][4].

IC50 & Target[1]

PPARγ

 

In Vitro

Netoglitazone (0.01-10 μM) induces the differentiation of U-33/γ2 cells into adipocytes in a concentration-dependent manner in vitro[1].
Netoglitazone (0.01-10 μM; 6 days) inhibits alkaline phosphatase activity in U-33/γ2 cells. A concentration higher than 1 μM is required for complete inhibition, and its potency after 6 days of treatment is at least 250-fold lower than that of rosiglitazone[1].
Netoglitazone (0.01-10 μM; 6 days) inhibits osteoblast mineralization in U-33/γ2 cells[1].
Netoglitazone (2 h) binds to PPARγ with an EC50 of 8 μM[3].

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

RT-PCR[1]

Cell Line: murine marrow-derived U-33/γ2 cells
Concentration: 2.5 μM
Incubation Time: 3 days
Result: Elevated FABP4/aP2 mRNA levels (adipocyte marker) at 2.5 μM.
Almost completely suppressed Runx2 mRNA levels (osteoblast marker) at 2.5 μM.
Matched the phenotypic effects of 0.5 μM rosiglitazone.
In Vivo

Netoglitazone (5-10 μg/g body weight/day; oral administration; once daily; for 4 consecutive days) exerts hypoglycemic effects comparable to those of rosiglitazone at 20 μg/g body weight/day in obese diabetic Avy mice, reducing fasting blood glucose by approximately 15-20%[1].
Netoglitazone maleate (10 μg/g body weight/day; oral administration; daily dosing for 7 weeks) alters fat depot weight and promotes bone marrow adipogenesis in non-diabetic male C57BL/6 mice, without affecting their trabecular bone microstructure or osteoblast gene expression, while causing a slight reduction in whole-body bone mineral content (BMC)[1].
Netoglitazone (1-30 mg/kg/day; p.o.; daily; for 4 consecutive days) potently reduces plasma glucose levels in obese diabetic KK-Ay mice, with an ED25 of 2.7 mg/kg/day, and regulates the expression of PPARγ-responsive genes in adipose tissue[3].

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

Animal Model: C57BL/6 mice (6-month-old male, non-diabetic)[1]
Dosage: 10 μg/g body weight/day
Administration: p.o.; daily; 7 weeks
Result: Did not affect body weight or blood glucose levels.
Decreased epididymal white adipose tissue (WAT) weight by 32.2%.
Increased interscapular brown adipose tissue (BAT) weight by 47.8%.
Left whole body bone mineral density (BMD) unchanged, but decreased whole body bone mineral content (BMC) by 4.6%.
Showed no changes in trabecular bone microarchitecture parameters (BV/TV, Tb.Th., Tb.N., Tb.Sp., Conn.D., SMI, DA) in the proximal tibia.
Increased marrow adipocyte number in the proximal tibia 3- to 6-fold.
Left expression of osteoblast-specific genes (Runx2, Dlx5, osteocalcin, α1(I) collagen) in the tibia unaffected, while increased adipocyte-specific gene FABP4/aP2 expression was increased 1.8-fold.
분자량

381.42

화학식

C21H16FNO3S

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(N1)SC(CC2=CC=C3C=C(OCC4=CC=CC=C4F)C=CC3=C2)C1=O

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 250 mg/mL (655.45 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 2.6218 mL 13.1089 mL 26.2178 mL
5 mM 0.5244 mL 2.6218 mL 5.2436 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (5.45 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 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 (5.45 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
순도&문서

Purity: 99.92%

References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6218 mL 13.1089 mL 26.2178 mL 65.5445 mL
5 mM 0.5244 mL 2.6218 mL 5.2436 mL 13.1089 mL
10 mM 0.2622 mL 1.3109 mL 2.6218 mL 6.5545 mL
15 mM 0.1748 mL 0.8739 mL 1.7479 mL 4.3696 mL
20 mM 0.1311 mL 0.6554 mL 1.3109 mL 3.2772 mL
25 mM 0.1049 mL 0.5244 mL 1.0487 mL 2.6218 mL
30 mM 0.0874 mL 0.4370 mL 0.8739 mL 2.1848 mL
40 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.6386 mL
50 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3109 mL
60 mM 0.0437 mL 0.2185 mL 0.4370 mL 1.0924 mL
80 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8193 mL
100 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6554 mL
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  • Do most proteins show cross-species activity?

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상품명:
Netoglitazone
Cat. No.:
HY-100428
수량:
MCE Japan Authorized Agent: