2. Cell Cycle/DNA Damage
    Vitamin D Related/Nuclear Receptor
  3. PPAR
  4. Chiglitazar

Chiglitazar  (Synonyms: Carfloglitazar)

Cat. No.: HY-106266 Purity: 96.66%
COA Handling Instructions

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

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

Chiglitazar Chemical Structure

Chiglitazar Chemical Structure

CAS No. : 743438-45-1

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Based on 1 publication(s) in Google Scholar

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  • References

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Description

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

IC50 & Target[1][2]

PPARα

1.8 μM (EC50)

PPARγ

0.08 μM (EC50)

PPARδ

1.7 μM (EC50)

In Vitro

Comparative dose-response study of Chiglitazar is performed with rosiglitazone and pioglitazone for PPARγ, and WY14643 for PPARα. Chiglitazar shows significant activation of both the isoforms. Chiglitazar shows weaker PPARγ activating activity than rosiglitazone, but stronger than pioglitazone. In terms of PPARα activation, Chiglitazar shows more potent activity than rosiglitazone, pioglitazone, or WY14643 which is a selective PPARα agonist[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

After insulin injection, plasma glucose levels in the MSG rats treated with Chiglitazar or rosiglitazone are significantly reduced compared with the control group treated with vehicle at all time points. Fasting PI levels are lower in animals treated with Chiglitazar and rosiglitazone than control. The ISIs of MSG obese rats treated with chiglitazar and rosiglitazone are significantly higher than control. Furthermore, Chiglitazar ameliorates the HOMA indices. For IPGTT, at the 30 min after glucose loading, the glucose values in the 5 and 10 mg /kg Chiglitazar and rosiglitazone-treatment groups are significantly lower than those in the vehicle treatment group. The integrated for the glucose response during the IPGTT in the treatment groups are significantly less than those in the control groups[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

572.62

Appearance

Solid

Formula

C36H29FN2O4
CAS No.
SMILES

O=C(C1=CC=C(F)C=C1)C(C=CC=C2)=C2N[[email protected]](C(O)=O)CC(C=C3)=CC=C3OCCN4C5=CC=CC=C5C6=CC=CC=C46
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (174.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7464 mL 8.7318 mL 17.4636 mL
5 mM 0.3493 mL 1.7464 mL 3.4927 mL
10 mM 0.1746 mL 0.8732 mL 1.7464 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: ≥ 2.5 mg/mL (4.37 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
Animal Administration
[1]

Rats[1]
MSG obese rats (6 months old) are sorted into five treatment groups (n=10 each, male and female in half) based on decreased blood glucose in the insulin tolerance test, glucose levels, blood total triglyceride (TG), total cholesterol (TCHO), and initial body weight. From the next day, MSG obese rats receive single daily oral treatment with Chiglitazar (5, 10, and 20 mg kg-1 day-1, respectively), rosiglitazone (5 mg kg-1 day-1) or vehicle (water, 0.05% Tween 80) for 40 days. Normal wistar rats (n=10) serve as a normal group are treated with vehicle[1].

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

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Keywords:

Chiglitazar743438-45-1CarfloglitazarPPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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