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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
37 Results for "
TSPO
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "TSPO" in MCE Product Catalog:
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PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
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4 Cited Publications
Synonyms: AC-5216; XBD-173
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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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1 Cited Publications
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ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment .
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1 Cited Publications
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DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=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 .
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PBR28 is a translocator protein (TSPO) binding positron emission tomography (PET) radiotracer with blood-brain barrier permeability . PBR28 binds to TSPO, a marker of microglial activation and neuroinflammation, and is used for neuroinflammation imaging in brain diseases and HIV-infected individuals .
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TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
Cat. No.: HY-400882
CAS No.: 958233-17-5
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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 Ki 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 .
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TSPO TRP Channel Microphthalmia Associated Transcription Factor (MITF) PKC PKA p38 MAPK PERK Interleukin Related
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FGIN-1-27 is a blood-brain barrier-penetrant TSPO ligand with a Ki value of 5 nM. FGIN 1-27 inhibits PKC-β, PKA/CREB, p38/ERK MAPK, MITF, tyrosinase, TRP-1, and TRP-2, thereby inhibiting melanogenesis and pigmentation. FGIN-1-27 alleviates X-ray radiation-induced astrocyte mitochondrial hyperfunction, reduces ROS and superoxide production, inhibits excessive activation of A1-type astrocytes, downregulates GFAP and C3 protein expression, and restores astrocyte proliferative capacity. FGIN-1-27 produces anticonvulsant effects in normal mice; in diazepam-withdrawn mice, the brain MDR pathway becomes subsensitive, and the anticonvulsant activity disappears. FGIN-1-27 attenuates pigmentation in zebrafish embryos and ameliorates UVB-induced skin pigmentation in guinea pigs. FGIN-1-27 directly stimulates testicular Leydig cells while upregulating luteinizing hormone levels, causing an acute increase in serum testosterone in male rats. FGIN 1-27 can be used for research related to hyperpigmentation, epilepsy, brain injury, and other diseases .
Cat. No.: HY-W782122
CAS No.: 1485490-47-8
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Photoclick cholesterol is a photoreactive cholesterol analog capable of undergoing click reactions. Photoclick cholesterol enables specific, saturable photoaffinity labeling of the mitochondrial translocator protein TSPO .
Cat. No.: HY-147225
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TSPO Ligand-Linker Conjugates 1 contains a ligand for translocator protein (TSPO) and a linker, which is used for the synthesis of mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC can bind the TSPO on the outer mitochondrial membrane (OMM) of mitochondria and degrades impaired mitochondria and proteins via mitophagy, and improves mitochondrial activity. TSPO Ligand-Linker Conjugates 1 can be used in mitochondrial dysfunction related research, including neurodegenerative diseases, cancer, and diabetes .
Cat. No.: HY-158408
CAS No.: 3062992-25-7
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NZ-66 is a ULK1-Recruiting Chimera (ULKREC) and heterobifunctional chimeric molecule composed of a BL-918-derived ULK1 agonist linked to a mitochondrial outer membrane-targeting TSPO ligand via a six-carbon hexane linker. NZ-66 is a mitophagy inducer recruits ULK1 to mitochondria to induce ULK1-dependent mitophagy, enhanced by mitochondrial insult, independently of the PRKN/PINK axis. NZ-66 can be used for the research of parkinson’s disease .
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 .
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(R)-ONO-2952 is a R-enantiomer of ONO-2952. ONO-2952 is a potent, selective and orally active TSPO antagonist with Kis of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes .
Synonyms: BIBD-239
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ER176 is a next generation PET radioligand for imaging 18 kDa translocator protein (TSPO), a biomarker for neuroinflammation .
Cat. No.: HY-175340
CAS No.: 1361107-81-4
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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 Ki 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 .
Cat. No.: HY-169964
CAS No.: 3116926-83-8
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TSPO/Carbonic Anhydrase Modulator 1 (Compound 3) is a dual modulator for mitochondrial translocator protein and Carbonic Anhydrase with a Ki of 1.340 μM for TSPO and a KA of 10.7 μM for CA VII. TSPO/Carbonic Anhydrase Modulator 1 promotes the production of neurosteroid, increases BDNF gene expression, exhibits neuroprotective efficacy .
Cat. No.: HY-RS15177
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TSPO Human Pre-designed siRNA Set A contains three designed siRNAs for TSPO gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS16721
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Tspo Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tspo gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS15178
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TSPO2 Human Pre-designed siRNA Set A contains three designed siRNAs for TSPO2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-150410
CAS No.: 2241669-89-4
TSPO ligand-3 is a ligand of AUTAC2. AUTAC2 contains an p-fluorobenzylguanine (FBnG) and an synthetic ligand of FKBP (SLF) moiety, which can cause significant silencing of FKBP12 in HeLa cells .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
