Thioperamide (Synonyms: MR-12842)

Name: Thioperamide
Brand: MedChemExpress
SKU: HY-12206
Rating: 4.5 (1 reviews)

Cat. No.: HY-12206 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

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Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [³H]histamine release. Thioperamide inhibits [³H]histamine synthesis with a K_i of 31 nM.

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

Thioperamide Chemical Structure

CAS No. : 106243-16-7

Size	Price	Stock	Quantity
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
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100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Thioperamide:

BYK 191023 dihydrochloride Get quote
Thioperamide maleate Get quote

1 Publications Citing Use of MCE Thioperamide

•Eur J Pharmacol. 2024 Jul 30:176866. [Abstract]

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

H₃ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	140 nM Compound: Thioperamide	Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay	[PMID: 30629436]
CHO-K1	IC₅₀	19 nM Compound: Thioperamide	Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay	[PMID: 31724859]
HEK293	IC₅₀	0.12 μM Compound: Thioperamide	Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay	[PMID: 23978359]
HEK293	EC₅₀	11 nM Compound: thioperamide	Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay	[PMID: 19553110]
HEK293	IC₅₀	517.5 nM Compound: T	Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay	[PMID: 22019465]
HEK293	IC₅₀	667 nM Compound: T	Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay	[PMID: 22019465]
SH-SY5Y	CC₅₀	85.79 μM Compound: Thioperamide	Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay	[PMID: 30822710]
U2OS	IC₅₀	1.03 μM Compound: Thioperamide	Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology	[PMID: 30822710]

In Vitro

Thioperamide inhibits [³H]-(R)α-MeHA binding rat brain and guinea-pig lung with K_is of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [³H]histamine release with a mean apparent K_i of 4 nM^[1].
Thioperamide (0.01-100 μM; 24 hours) promotes the viability of NE-4C stem cells in a concentration-dependent manner^[2].

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

Cell Viability Assay^[2]

Cell Line:	NE-4C stem cells
Concentration:	0.01, 0.1, 1, 10, 100 μM
Incubation Time:	24 hours
Result:	The viability of NE-4C stem cells increased significantly to 150.83±6.91% when (1 μM) was administrated, and increased to 145.11±14.52% and 132.02%±25.65% when 10 μM and 100 μM were administrated respectively.

In Vivo

Thioperamide (5-20 mg/kg; i.p.) is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice^[3].

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

Animal Model:	Naive female C57BL/6J mice^[3]
Dosage:	5, 10 or 20 mg/kg
Administration:	Injections (i.p.)
Result:	Facilitated reconsolidation of a contextually-conditioned fear memory.

Molecular Weight

292.44

Formula

C₁₅H₂₄N₄S

CAS No.

106243-16-7

Appearance

Solid

Color

White to off-white

SMILES

S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (341.95 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	3.4195 mL	17.0975 mL	34.1950 mL
5 mM	0.6839 mL	3.4195 mL	6.8390 mL
10 mM	0.3420 mL	1.7098 mL	3.4195 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. 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 2.5 mg/mL (8.55 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (8.55 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (8.55 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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

Purity: 99.91%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) HNMR (141 KB) RP-HPLC (168 KB) LCMS (412 KB)

Handling Instructions (2659 KB)

References

[1]. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23. [Content Brief]

[2]. Na Wang, et al. Histamine H3 Receptor Antagonist Enhances Neurogenesis and Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairments. Front Pharmacol. 2020 Jan 21;10:1583. [Content Brief]

[3]. Y Charlier, et al. Differential Effects of Histamine H(3) Receptor Inverse Agonist Thioperamide, Given Alone or in Combination With the N-methyl-d-aspartate Receptor Antagonist Dizocilpine, on Reconsolidation and Consolidation of a Contextual Fear Memory [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4195 mL	17.0975 mL	34.1950 mL	85.4876 mL
	5 mM	0.6839 mL	3.4195 mL	6.8390 mL	17.0975 mL
	10 mM	0.3420 mL	1.7098 mL	3.4195 mL	8.5488 mL
	15 mM	0.2280 mL	1.1398 mL	2.2797 mL	5.6992 mL
	20 mM	0.1710 mL	0.8549 mL	1.7098 mL	4.2744 mL
	25 mM	0.1368 mL	0.6839 mL	1.3678 mL	3.4195 mL
	30 mM	0.1140 mL	0.5699 mL	1.1398 mL	2.8496 mL
	40 mM	0.0855 mL	0.4274 mL	0.8549 mL	2.1372 mL
	50 mM	0.0684 mL	0.3420 mL	0.6839 mL	1.7098 mL
	60 mM	0.0570 mL	0.2850 mL	0.5699 mL	1.4248 mL
	80 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0686 mL
	100 mM	0.0342 mL	0.1710 mL	0.3420 mL	0.8549 mL

Thioperamide Related Classifications

Neurological Disease

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.

Keywords:

Thioperamide106243-16-7MR-12842MR12842MR 12842Histamine ReceptorH3receptorreleasehistaminesynthesisParkinsonInhibitorinhibitorinhibit

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Thioperamide (Synonyms: MR-12842)

Customer Review

Other Forms of Thioperamide:

Thioperamide Related Antibodies

1 Publications Citing Use of MCE Thioperamide

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Thioperamide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Thioperamide Related Classifications

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