2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Thioperamide maleate

Thioperamide maleate  (Synonyms: MR-12842 maleate)

Cat. No.: HY-12206A Purity: 98.26%
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Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM.

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Thioperamide maleate Chemical Structure

Thioperamide maleate Chemical Structure

CAS No. : 148440-81-7

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Based on 1 publication(s) in Google Scholar

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Thioperamide maleate Related Antibodies

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Description

Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM[1].

IC50 & Target[1]

H3 Receptor

 

In Vitro

Thioperamide inhibits [3H]-(R)α-MeHA binding rat brain and guinea-pig lung with Kis of 2.1 nM and 2.0 nM, respectively. Thioperamide competitively blocks H3-autoreceptors regulating [3H]histamine release with a mean apparent Ki 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].
Thioperamide displays similar potencies at human H4 and H3 receptors (Ki=43 and 60 nM, respectively)[3].

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

Thioperamide maleate Related Antibodies

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[4].

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

Animal Model: Naive female C57BL/6J mice[4]
Dosage: 5, 10 or 20 mg/kg
Administration: Injections (i.p.)
Result: Facilitated reconsolidation of a contextually-conditioned fear memory.
Formula

C15H24N4S.xC4H4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

S=C(N1CCC(C2=CN=CN2)CC1)NC3CCCCC3.O=C(O)/C=C\C(O)=O.[x]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (Need ultrasonic)

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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Thioperamide maleate Related Classifications

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:

Thioperamide148440-81-7MR-12842MR12842MR 12842Histamine ReceptorInhibitorinhibitorinhibit

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