Fig. 1 · Structure

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Trospium chloride

mAChR Inhibitor

Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling.

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In Vitro Studies

Trospium chloride was evaluated in HEK-OCT2 cells for inhibition of OCT2-dependent metformin uptake. The reported IC50 was 0.07 μM. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Inhibition of metformin uptake in HEK-OCT2 cells

Cell-based study · HEK-OCT2 cells; n = 6 [1]

In HEK-OCT2 cells, Trospium chloride inhibited OCT2-dependent uptake of metformin with an IC50 of 0.07 μM.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
IC50 values for inhibition of OCT2-dependent uptake of metforminIC50 0.07 μM[1]

Literature-Reported Treatment Conditions

Exposure duration
37°C for 3 min
Method
in the presence of increasing concentrations of test drugs
Reported limits
Not stated in the sentences used: dose, vehicle.
Methods and source locations

Compound reported in the paper: Trospium chloride

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Transport Assays in HEK-OCT2 Cells (S15, S17, S18); Materials and Methods > IC50 Determination (S31, S32, S35); Fig 5 legend (S112); Table 1 legend (S114); Table 1 (T1.h1, T1.r8)

IC50 values for inhibition of OCT2-dependent uptake of metformin: IC50 values for inhibition of OCT2-dependent uptake of metformin; comparator: net uptake in the absence of the inhibitor — Table 1 legend (S114); Table 1 (T1.h1, T1.r8)

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 10405-02-4
Applications mAChR Inhibitor
Formula C25H30ClNO3
Molecular Weight 427.96
SMILES
[H][C@@]12CC[C@@](C[C@@H](OC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)=O)C2)([H])[N+]15CCCC5.[Cl-]

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Hacker K, Maas R, Kornhuber J, et al. Substrate-Dependent Inhibition of the Human Organic Cation Transporter OCT2: A Comparison of Metformin with Experimental Substrates. PLoS One (2015). PMID: 26327616 DOI: 10.1371/journal.pone.0136451 Source material

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