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  3. Progoitrin

Progoitrin is a sulfur-containing glucosinolate, as well as a naturally occurring orally active thioglycoside. Progoitrin acts as a hepatotoxin and antithyroid agent. Progoitrin is quantitatively converted to goitrin in vivo, including via a gastrointestinal hydrolysis pathway that does not require exogenous myrosinase, thereby blocking the organification of iodine in the thyroid gland and inhibiting the uptake and accumulation of radioactive iodine. Progoitrin can be used in studies related to Graves' disease.

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Progoitrin

Progoitrin Chemical Structure

CAS No. : 585-95-5

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Description

Progoitrin is a sulfur-containing glucosinolate, as well as a naturally occurring orally active thioglycoside. Progoitrin acts as a hepatotoxin and antithyroid agent. Progoitrin is quantitatively converted to goitrin in vivo, including via a gastrointestinal hydrolysis pathway that does not require exogenous myrosinase, thereby blocking the organification of iodine in the thyroid gland and inhibiting the uptake and accumulation of radioactive iodine. Progoitrin can be used in studies related to Graves' disease[1][2][3].

In Vitro

Progoitrin does not block organic binding of iodine in in vitro thyroid slice assays[2].

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

In Vivo

Progoitrin (20-300 mg; p.o.; single dose) dose-dependently inhibits thyroidal 131I uptake in male Holtzman rats, with higher doses and shorter intervals between progoitrin administration and 131I exposure producing greater suppression of uptake[2].
Progoitrin (p.o.; s.c.; i.p.; single dose) exhibits greater antithyroid potency than systemic (subcutaneous or intraperitoneal) progoitrin at lower doses in male Holtzman rats on a low iodine diet, with larger oral doses showing reduced efficacy due to gastrointestinal intolerance[2].

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

Animal Model: Holtzman (male, 100-120 Gm)[2]
Dosage: 20 mg; 100 mg; 200 mg; 300 mg
Administration: p.o.; single dose
Result: Reduced thyroidal I131 uptake to 42.9% of controls (300 mg, 23.5 hours before I131).
Molecular Weight

389.40

Formula

C11H19NO10S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=C[C@H](O)C/C(S[C@@H]1O[C@@H]([C@H]([C@@H]([C@H]1O)O)O)CO)=N/OS(=O)(O)=O

Structure Classification
Initial Source
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 : 10 mg/mL (25.68 mM; ultrasonic and warming and heat to 60°C; 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 2.5681 mL 12.8403 mL 25.6805 mL
5 mM 0.5136 mL 2.5681 mL 5.1361 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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: ≥ 1 mg/mL (2.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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

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(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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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 (sealed storage, away from moisture and light). 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 2.5681 mL 12.8403 mL 25.6805 mL 64.2013 mL
5 mM 0.5136 mL 2.5681 mL 5.1361 mL 12.8403 mL
10 mM 0.2568 mL 1.2840 mL 2.5681 mL 6.4201 mL
15 mM 0.1712 mL 0.8560 mL 1.7120 mL 4.2801 mL
20 mM 0.1284 mL 0.6420 mL 1.2840 mL 3.2101 mL
25 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5681 mL
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  • 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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Progoitrin
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