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TSHR antagonist S37a

Name: TSHR antagonist S37a
Brand: TargetMol
SKU: T13217
Rating: 4.5 (1 reviews)

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Catalog No. T13217Cas No. 2143452-20-2

TSHR antagonist S37a is a selective, orally bioavailable TSHR (thyroid-stimulating hormone receptor) antagonist that inhibits TSH-induced cyclic adenosine monophosphate (cAMP) in TSHR-expressing HEK 293 cells, suitable for studying Graves' orbitopathy.

TSHR antagonist S37a

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Catalog No. T13217Cas No. 2143452-20-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$152	6-8 weeks	6-8 weeks
5 mg	$378	6-8 weeks	6-8 weeks
10 mg	$596	6-8 weeks	6-8 weeks
25 mg	$1,160	6-8 weeks	6-8 weeks
50 mg	$1,730	6-8 weeks	6-8 weeks
100 mg	$2,530	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$385	6-8 weeks	6-8 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	TSHR antagonist S37a is a selective, orally bioavailable TSHR (thyroid-stimulating hormone receptor) antagonist that inhibits TSH-induced cyclic adenosine monophosphate (cAMP) in TSHR-expressing HEK 293 cells, suitable for studying Graves' orbitopathy.
In vitro	In HEK293 cells, TSHR antagonist S37a exhibits inhibitory activity against TSHR: its IC₅₀ for mTSHR is 40 μM, while the IC₅₀ for hTSHR is approximately 20 μM [1]. TSHR antagonist S37a not only inhibits the activation of TSHR by thyrotropin itself but also suppresses the activation of TSHR by monoclonal TSAbs (including the Homo sapiens-derived antibody M22 and the murine-derived antibody KSAb1) as well as the Broussonetia papyrifera-derived small-molecule agonist C2 [1].
In vivo	The TSHR antagonist S37a can inhibit the cyclic adenosine monophosphate (cAMP) production induced by oligoclonal TSAbs (thyroid-stimulating hormone receptor-stimulating antibodies), and these oligoclonal TSAbs are highly enriched in the serum of patients with Graves' ophthalmopathy (GO) [1]. When administered via oral gavage at a dose of 10 mg/kg, the TSHR antagonist S37a exhibited no toxicity in mice and demonstrated a significant oral bioavailability of 53% [1].

Chemical Properties

Molecular Weight	460.57
Formula	C₂₅H₂₀N₂O₃S₂
Cas No.	2143452-20-2
Smiles	O=C1[C@@]2([C@@]3([C@@]4([C@]([C@@](C3)([C@@]2(C(=O)N1C5=CC=CC=C5)[H])[H])(SC6=C([C@H]4C7=CC=CC=C7)SC(=O)N6)[H])[H])[H])[H]
Relative Density.	1.54 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (173.7 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1712 mL	10.8561 mL	21.7122 mL	108.5611 mL
5 mM	0.4342 mL	2.1712 mL	4.3424 mL	21.7122 mL
10 mM	0.2171 mL	1.0856 mL	2.1712 mL	10.8561 mL
20 mM	0.1086 mL	0.5428 mL	1.0856 mL	5.4281 mL
50 mM	0.0434 mL	0.2171 mL	0.4342 mL	2.1712 mL
100 mM	0.0217 mL	0.1086 mL	0.2171 mL	1.0856 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc