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UK-101
UK101, UK 101
T132471000313-40-5In house
UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM, respectively. UK-101 exhibits a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer-related diseases.
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6-8weeks
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TargetMol | Inhibitor Hot
Theophylline monohydrate
Quibron
T1083L5967-84-0
Theophylline monohydrate (Quibron) appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline monohydrate is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologically, this agent relaxes the bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates the cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.
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4-Hydroxyantipyrine
T22251672-63-5
4-Hydroxyantipyrine is formed during oxidative deamination of aminopyrine.
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7-Methoxy-1-naphthaleneacetic acid
T98976836-22-2
7-Methoxy-1-naphthaleneacetic acid is an inhibitor of auxin action in plants. 7-Methoxy-1-naphthaleneacetic acid inhibits polar auxin transport and tropic responses associated with asymmetric auxin distribution in Arabidopsis and maize. 7-Methoxy-1-naphthaleneacetic acid inhibits auxin transport mediated by AUX1, PIN, and ABCB proteins expressed in yeast.
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INOSINIC ACID
Inosine 5′-monophosphate, IMP, I-5'-P
T4685131-99-7
Inosinic acid (IMP) is a purine nucleotide which has hypoxanthine as the base and one phosphate group esterified to the sugar moiety. Inosinic acid is a nucleotide present in muscle and other tissues. It is formed by the deamination of AMP and when hydrolysed produces inosine. Inosinic acid is the ribonucleotide of hypoxanthine and is the first compound formed during the synthesis of purine.Inosine 5′-monophosphate (IMP) is used as a substrate to study the distribution, specificity and kinetics of inosine-5′-monophosphate dehydrogenase (IMPDH).
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Recilisib sodium
Brand name: Ex-RAD,ON 01210.Na,ON01210,ON-01210
T13862L922139-31-9
Recilisib, also known as ON 01210.Na, is a radioprotectant, which modifys cell cycle distribution patterns in cancer cells subjected to radiation therapy, and it has been identified as a potential candidate for radiation protection studies. It appears tha
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1-2 weeks
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Anguizole
T14289442666-98-0
Anguizole, a small molecule, effectively inhibits Hepatitis C Virus (HCV) replication by modifying the subcellular distribution of NS4B. It demonstrates its potency with an IC50 value, highlighting its specific target action against HCV.
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7-10 days
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Taribavirin hydrochloride
T1699240372-00-7
Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor designed to concentrate within the liver to target HCV-infected hepatocytes, while minimizing distribution within red blood cells and the development of hemolytic anemia [2].
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6-8 weeks
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Taribavirin
T16993119567-79-2
Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor designed to concentrate within the liver to target HCV-infected hepatocytes, while minimizing distribution within red blood cells (RBCs) and thereby reducing the risk of developing hemolytic anemia.
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6-8 weeks
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Ferroptosis-IN-12
T200665
Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia reperfusion (I R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.
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1-1(Z)-Octadecenyl-2-docosahexaenoyl-sn-glycero-3-PE
18:0p 22:6-PE
T201867206059-98-5
1-1(Z)-Octadecenyl-2-docosahexaenoyl-sn-glycero-3-PE (18:0p 22:6-PE) is a lipid identified in rat brain tissue using mass spectrometry imaging techniques. It exhibits specific structural and distribution properties, allowing the differentiation of isomers of various fatty acid chains through refined methods.
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PF-07265028
PF07265028, PF 07265028
T2023432736458-30-1
PF-07265028 is an HPK1 inhibitor with an IC50 of 17 nM. Pharmacokinetic studies in mice and monkeys indicate that PF-07265028 exhibits moderate clearance, terminal half-life, volume of distribution, and oral bioavailability. It targets, binds, and inhibits Hpk1 activity, blocking Hpk1-mediated signaling pathways to prevent immune suppression mediated by Hpk1, including the inhibition of T-cell receptor (TCR) signaling, effector T-cell suppression, aberrant cytokine expression, and the elimination of the immunosuppressive tumor microenvironment (TME). This action can activate a cytotoxic T lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1 is primarily expressed in hematopoietic cells and acts as a negative regulator of TCR signaling and T and B cell activation.
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Stilbamidine dihydrochloride
NSC 35605,NCI 174
T262306935-63-3
Stilbamidine dihydrochloride is a blocker of neuromuscular transmission and axonal conduction used to study the distribution of the drug in the organs and tissues of rats following intravenous injection.
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7-10 days
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WB403
WB-403,WB 403
T291541594041-84-5
WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-
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6-8 weeks
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Arbaclofen placarbil
XP 19986,XP19986,XP-19986
T30118847353-30-4
Arbaclofen placarbil( XP19986) is a GABA(B) receptor agonist.Arbaclofen Placarbil is a novel R-baclofen prodrug with improved absorption, distribution, metabolism, and elimination properties compared to R-baclofen. And it can reduce postprandial reflux in
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6-8 weeks
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Histidyl-aspartyl-glutamyl-leucine
His-asp-glu-leu,Hdel sequence
T32082129623-52-5
HDEL intracellular distribution is characteristic of plant endoplasmic reticulum (ER).
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MIP-1095 I-123
123-I-MIP-1095, (123I)MIP 1095
T33392949575-25-1
MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents).
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PROTAC_ERRalpha
T34166
PROTAC_ERRalpha is a proteolysis targeting chimeras (PROTAC) which provides broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts.
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Teduglutide acetate
T35337L
Teduglutide acetate, a GLP-2 analogue, maximizes small intestinal mucosal hypertrophy. Teduglutide acetate partially restores small intestinal epithelial function through an altered distribution of claudin-10, facilitating sodium recirculation for Na-coupled glucose transport and water absorption.
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10-Thiastearic Acid
T35448105099-89-6
Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.
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Pentosidine
T35890124505-87-9
Advanced glycation end products (AGEs) are compounds formed by non-enzymatic chemical reactions following the bonding of sugars to proteins or lipids during diabetes, uremia, aging, rheumatic arthritis, and other conditions. A receptor for the AGEs (RAGE) binds certain members of this class to initiate cell signaling.[1][2] Pentosidine is a well-characterized natural AGE that is often used as a biomarker for the production of all AGEs. While pentosidine can be measured in urine, the majority of this AGE is catabolized before excretion.[3] Reference:[1]. Neeper, M., Schmidt, A.M., Brett, J., et al. Cloning and expression of a cell surface receptor for advanced glycosylation end products of proteins. The Journal of Biological Chemisty 267(21), 14998-15004 (1992).[2]. Brett, J., Schmidt, A.M., Yan, S.D., et al. Survey of the distribution of a newly characterized receptor for advanced glycation end products in tissues. American Journal of Pathology 143(6), 1699-1712 (1993).[3]. Miyata, T., Ueda, Y., Horie, K., et al. Renal catabolism of advanced glycation end products: The fate of pentosidine. Kidney International 53, 416-422 (1998).
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Resolvin D1 methyl ester
Resolvin D1 methyl ester
T37168937738-63-1
Resolvin D1 is produced physiologically from the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase . It reduces human polymorphonuclear leukocyte transendothelial migration, the earliest event in acute inflammation, with an EC50 value of ~30 nM. RvD1 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.
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10-14 weeks
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Resolvin D2 methyl ester
T37169810668-53-2
Resolvin D2 (RvD2) is a lipid mediator biosynthesized by the sequential oxygenation of docosahexaenoic acid by 15- and 5-lipoxygenase. It evokes diverse anti-inflammatory effects which may mediate the resolution of inflammation. RvD2 methyl ester is a methyl ester version of the free acid which may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.
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Resolvin D3 methyl ester
T37290
Resolvin D3 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.
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