TSPO

Translocator Protein

TSPO (Translocator Protein) is a conserved membrane protein located on the outer mitochondrial membrane of eukaryotic cells, with the 18 kDa subtype being the most studied in mammals. It regulates steroid synthesis, mitochondrial function, apoptosis, and immune responses, influencing mitochondrial membrane permeability, energy metabolism, and cellular stress through pathways such as PKA, MAPK, and NF-κB. TSPO plays a significant role in neurodegenerative diseases (e.g., Alzheimer's, Parkinson's), psychiatric disorders (e.g., anxiety, depression), cancer, and inflammatory diseases, with its altered expression making it a potential target for diagnosis and therapy^[1].

TSPO Related Products (10):

By Effects:	Inhibitors (3) Ligands (2) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-15527

Emapunil	Inhibitor	99.94%
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models.

HY-400882

Tosylate-DPA-714	Ligand	98.78%
Tosylate-DPA-714 is a GMP-grade precursor for the radiosynthesis of DPA-714 (HY-122607). It crosses the blood-brain barrier and exhibits steroidogenic activity. DPA-714 is a specific ligand for the 18 kDa translocator protein (TSPO) with a K_i of 7.0 nM. Tosylate-DPA-714 is safe and does not bind to central benzodiazepine receptors (benzodiazepine receptor). As a radiolabeling precursor, Tosylate-DPA-714 reacts with ¹⁸F via nucleophilic aliphatic substitution to form ¹⁸F-DPA-714, enabling specific targeted binding to TSPO. ¹⁸F-DPA-714 accurately reflects the level of neuroinflammation mediated by microglial activation, and is used for PET molecular imaging of neurological diseases such as Alzheimer's disease and multiple sclerosis.

HY-122607

DPA-714		99.86%
DPA-714 is a high affinity translocator protein (TSPO) ligand (K_i=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. ^18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.

HY-150409

TSPO ligand-2	Ligand	99.63%
TSPO ligand-2 is a ligand of AUTAC1. AUTAC1 contains an p-fluorobenzylguanine (FBnG) and a Fumagillol moiety, which can silence endogenous MetAP2 in HeLa cells.

HY-175340

Kv7.2/Kv7.3 activator-3	Activator
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC₅₀ values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with K_i values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons.

HY-122607S

DPA-714-d₁₀
DPA-714-d₁₀ is the deuterium labeled DPA-714 (HY-122607). DPA-714 is a high affinity translocator protein (TSPO) ligand (K_i=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. ¹⁸FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.

HY-172534

BPN-01
BPN-01 is a fluorescent probe targeting translocator protein (TSPO) and human epidermal growth factor receptor 2 (HER2) with binding affinities of -10.7 kcal/mol for TSPO and -11.3 kcal/mol for HER2. BPN-01 is promising for research of solid tumor imaging during fluorescence image-guided surgery (FIGS) (Ex/Em = 475/510 nm).

HY-19854

TRO-40303
TRO-40303 is a cell protective compound targeting mitochondrial TSPO. TRO-40303 significantly improves the survival rate of liver cells and reduces cell death by reducing oxidative stress. TRO-40303 is commonly used in the study of hepatitis.

HY-161490

AMOZ/BSA	Inhibitor
AMOZ/BSA is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

HY-15527R

Emapunil (Standard)	Inhibitor
Emapunil (Standard) is the analytical standard of Emapunil. This product is intended for research and analytical applications. Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models.

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