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Art. -Nr.: HY-178393

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TRPM2-IN-2

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC₅₀ = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC₅₀ >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₄H₂₉N₃O₂
Molecular Weight:391.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

TRPM2-IN-2 Chemical Structure

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

TRPM2

0.66 μM (IC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

In Vitro

TRPM2-IN-2 (LC4) (0.03-10 μM, 6-24 h) shows protective effects of adamantane derivatives on an OGD/R cell model, with low cytotoxicity in SH-SY5Y cells^[1].
TRPM2-IN-2 (10 μM) exhibits minimal inhibition activity against TRPV1 and TRPM8 with inhibition rates of 20.5% and 23.2%^[1].
TRPM2-IN-2 inhibits hERG channel with an IC₅₀ of 21.61 μM in CHO cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

SH-SY5Y cells
Concentration:

0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time:

6 and 24 h
Result:

Showed low cytotoxicity in SH-SY5Y cells at 10 μM.
Showed no significant cytotoxicity in SH-SY5Y cells up to 1 μM.
Exhibited significant protective effects against OGD/R-induced injury at 0.1 μM and notably maintaining protection even at 0.03 μM.
Did not exhibit significant cytotoxicity at its effective concentration (0.03-0.3 μM).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	CL	MRT	F
Rat^[1]	1 mg/kg	i.v.	2.74 h	0.08 h	3560.87 ng/mL	1375.65 ng·h/mL	1375.94 ng·h/mL	15.09 mL/min/kg	2.19 h	/
Rat^[1]	10 mg/kg	i.g.	5.56 h	0.08 h	1443.47 ng/mL	896.98 ng·h/mL	1320.73 ng·h/mL	21.70 mL/min/kg	5.73 h	9.60 %

In Vivo

TRPM2-IN-2 (0.3, 1 and 3 mg/kg, i.v., single dose at 3 h post-reperfusion) shows significant neuroprotective effects in the tMCAO mouse model^[1].

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

Animal Model:

Male C57BL/6J mice (8-10 weeks) subjected to 1 h of ischemia followed by 3 h of reperfusion^[1]
Dosage:

0.3, 1 and 3 mg/kg
Administration:

i.v., single dose at 3 h post-reperfusion
Result:

Significantly reduced infarct volume (35.7 %) compared with the vehicle group (60.9 %) at 3 mg/kg.
Exhibited comparable efficacy to 3 mg/kg of Edaravone (HY-B0099) at 1 mg/kg.
Did not show significant protection at 0.3 mg/kg.
Had significantly better outcomes than the vehicle at 3 mg/kg.
Showed no significant improvement compared with vehicle at 0.3 and 1 mg/kg.
significantly lowered levels of MDA (6.8 μM/mgprot) and LDH (0.18 U/mgprot).

Related Protocols :

How to Choose the Right Model Animal

Chemical Information

Molecular Weight 391.51
Formel C₂₄H₂₉N₃O₂
SMILES

O=C(N1CCCC1)C2=CC3=CC=CN3C(C(NC4(C[C@H]5C6)C[C@H]6C[C@H](C5)C4)=O)=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lu T, et al. Discovery of adamantyl derivatives as potent and selective TRPM2 inhibitors with significantly reduced hERG liability. Eur J Med Chem. 2025 Dec 15;300:118172. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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