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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

😃Good

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
Relative Density.	1.54 g/cm3 (Predicted)
Color	Yellow
Appearance	Solid

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 recommeded.

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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