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  3. Saroglitazar magnesium

Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

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Saroglitazar magnesium

Saroglitazar magnesium 화학구조

CAS No. : 1639792-20-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
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

Based on 10 publication(s) in Google Scholar

Other Forms of Saroglitazar magnesium:

Top Publications Citing Use of Products

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  • Biological Activity

  • Protocol

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

IC50 & Target[1]

PPARα

0.65 pM (EC50, HepG2 cell)

PPARγ

3 nM (EC50, HepG2 cell)

In Vivo

In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel therapeutic agent for treatment of dyslipidemia and diabetes[1].

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

Clinical Trial
분자량

901.42

화학식

C50H56MgN2O8S2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCO([Mg+2]1(O(CC)[C@H](C([O-]1)=O)CC2=CC=C(OCCN3C(C)=CC=C3C4=CC=C(SC)C=C4)C=C2)[O-]C5=O)[C@H]5CC6=CC=C(OCCN7C(C)=CC=C7C8=CC=C(SC)C=C8)C=C6

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : 125 mg/mL (138.67 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 1.1094 mL 5.5468 mL 11.0936 mL
5 mM 0.2219 mL 1.1094 mL 2.2187 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.75 mg/mL (3.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: 2.75 mg/mL (3.05 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.75 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 (27.5 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).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

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: 98.85%

References
Animal Administration
[1]

Rats: Rats randomize based on body weights and are divided into three equal groups and receives the daily administration of vehicle (50% w/v honey for marmoset and 0.1% carboxymethylcellulose for Wistar rats) or Saroglitazar (1.5 and 15 mg/kg per day) for 90 days by oral gavage[1].

Mice: Male C57BL/6J-db/db mice are bled on day 0 to determine pretreatment serum glucose and TG. During next 12 days, each animal is dosed (by oral gavage) with vehicle (0.5% sodium carboxymethyl cellulose) or Saroglitazar (0.01, 0.03, 0.1, 0.3,1, and 3 mg/kg per day) or U 72107 (60 mg/kg per day) and on day 12 of the treatment, blood samples are collected (1 h after dosing) from orbital sinus under light ether anesthesia. The serum is isolated and analyzed for glucose, TG, and free fatty acid (FFA)[1].

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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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1094 mL 5.5468 mL 11.0936 mL 27.7340 mL
5 mM 0.2219 mL 1.1094 mL 2.2187 mL 5.5468 mL
10 mM 0.1109 mL 0.5547 mL 1.1094 mL 2.7734 mL
15 mM 0.0740 mL 0.3698 mL 0.7396 mL 1.8489 mL
20 mM 0.0555 mL 0.2773 mL 0.5547 mL 1.3867 mL
25 mM 0.0444 mL 0.2219 mL 0.4437 mL 1.1094 mL
30 mM 0.0370 mL 0.1849 mL 0.3698 mL 0.9245 mL
40 mM 0.0277 mL 0.1387 mL 0.2773 mL 0.6934 mL
50 mM 0.0222 mL 0.1109 mL 0.2219 mL 0.5547 mL
60 mM 0.0185 mL 0.0924 mL 0.1849 mL 0.4622 mL
80 mM 0.0139 mL 0.0693 mL 0.1387 mL 0.3467 mL
100 mM 0.0111 mL 0.0555 mL 0.1109 mL 0.2773 mL
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상품명:
Saroglitazar magnesium
Cat. No.:
HY-19937A
수량:
MCE Japan Authorized Agent: