co-2

2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan is a drug-linker conjugate for ADCs, featuring a cleavable linker coupled to Exatecan. This specific compound can be conjugated to the anti-Her3 antibody [1].

Co 101244 hydrochloride (4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride) is an NR2B-containing NMDA receptor antagonist.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Cetyl glycol (NSC-71525) favors the decomposition of the metal-organic precursor, formation of an intermediate Co(2+)Fe(3+)-oleate complex, and the nucleation of nanoparticles at lower temperatures. Cetyl glycol is a reducing agent that can be used in cosmetics.

Mitiglinide calcium hydrate (S-21403 calcium hydrate) is a drug for the treatment of type 2 diabetes. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs and is currently co-marketed in Japan by Kissei and Takeda.

Sotagliflozin (LP-802034) is an orally bioavailable inhibitor of the sodium-glucose co-transporter subtype 1 (SGLT1) and 2 (SGLT2), with potential antihyperglycemic activity.

Mazdutide acetate is a potent co-agonist of glucagon-like peptide (GLP-1R) and glucagon receptor (GCGR), a gastrin-regulating hormone analog.Mazdutide acetate stimulates insulin secretion from mouse pancreatic islets, and can be used in studies of obesity and type 2 diabetes (T2D).

BChE HDAC6-IN-2 is a selective and potent dual inhibitor of BChE and HDAC6 with neuroprotective and reactive oxygen species (ROS) scavenging activity. BChE HDAC6-IN-2 is a metal ion co-agonist that inhibits tau phosphorylation and can be used in the study of immune and neurological diseases.

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (PF-05231023) is a long-acting fibroblast growth factor 21 (FGF21) analog and FGF21-receptor agonist, suitable for development as a potential treatment for T2DM.

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl Prkl family of serine threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

Cetilistat (ATL-962) is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes.

Phosphoenolpyruvate carboxylase (PEPC) is an enzyme that irreversibly catalyzes the conversion of phosphoenolpyruvate and bicarbonate to oxaloacetate and inorganic phosphorus in the presence of Mg2+. It is essential for the primary assimilation of CO(2) in Crassulacean acid metabolism plants and significantly influences the diurnal rhythm of plant metabolism [1] [2].

Cyclic di-IMP (sodium salt) (c-di-IMP) is a synthetic second messenger structurally related to the bacterial second messengers cyclic di-GMP and cyclic di-AMP . C-di-IMP has adjuvant properties when co-administered with antigens in vitro and by mucosal routes in vivo. C-di-IMP enriches the population of MHC class I and II, CD80, CD86, CD40, and CD54 positive dendritic cells derived from murine bone marrow. It also stimulates macrophages at 500 ng/ml. Mice immunized with β-galactosidase (β-gal) plus c-di-IMP through the intranasal route show a humoral immune response, evidenced by an increase in IgG titers up to 2-fold compared to mice immunized with β-gal alone. Mice immunized with β-gal plus c-di-IMP also exhibit a Th1/Th2 response, indicating that the adjuvant activity of c-di-IMP leads to a cellular immune response as well.

D-Ribofuranose (D-Ribose), an endogenous metabolite found in cerebrospinal fluid, serves as a research tool for studying Ribose 5 Phosphate Isomerase Deficiency and Medium Chain Acyl Co A Dehydrogenase Deficiency [1] [2].

1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) exhibits vasodilator action through an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx via L-type voltage-operated Ca(2+) channels. A minor contribution to HM-1's effects may stem from inhibiting protein kinase C-mediated release of intracellular Ca(2+) stores. At 1 µg mL, HM-1 effectively inhibits osteoclast differentiation in co-cultures with mouse osteoblastic calvarial and bone marrow cells and protects mice from acute lung injury induced by lipopolysaccharide (LPS), likely by increasing IκB-α protein expression and suppressing inducible nitric oxide synthase and cyclooxygenase-Ⅱ protein expression.

AMD-3329 hydrobromide is a biochemical in the class of potent and selective anti-HIV-1 and HIV-2 agents that inhibit virus replication by binding to the chemokine receptor CXCR4, the co-receptor for entry of X4 viruses.

Caricotamide is a synthetic co-substrate that activates the human endogenous enzyme NRH:quinone oxidoreductase 2 (NQO2) with potential chemoadjuvant activity. When caricotamide is administered simultaneously with the prodrug tretazicar, NQO2 converts tretazicar to the bifunctional alkylating agent dinitrobenzamide, which is capable of forming a high degree of DNA interstrand cross-links, resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be over-expressed in cancers such as hepatocellular carcinoma (HCC), colorectal and ovarian cancers.

CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.

Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker conjugate utilized in PAC, comprising the BRD4 degrader GNE-987 connected with a 3-PEG linker. This compound serves as a click chemistry reagent, featuring an Azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules containing an Alkyne group. Additionally, it can participate in strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules that possess DBCO or BCN groups.

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthetic E3 ligase ligand-linker conjugate composed of a VHL ligand and a linker, utilized in PROTAC BRD4 Degrader-5 and PROTAC BRD4 Degrader-5-CO-PEG3-N3.

Nur77 modulator 2 is a Nur77 regulator with a Kd value of 0.35 μM. Nur77 modulator 2 is also a potent, orally active inhibitor of inflammation. nur77 modulator 2 regulates Nur77 co-localization in mitochondria.

Leriglitazone, a metabolite of pioglitazone, binds to the PPARγ C-terminal ligand-binding domain (Ki: 1.2 μM) and induces transcriptional efficacy of the PPARγ (EC50: 680 nM). Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation functio

AZD-CO-C2-Ph-amido-Ph-azide is an alkyl chain-derived PROTAC linker suitable for the synthesis of PROTACs [1].

photoCORM-2 is a single carbon monoxide releasing molecule (CORM). photoCORM-2 exhibits good cellular uptake and real-time monitoring ability of CO uncaging by a color change approach. photoCORM-2 has anti-tumor activity .

1. beta-Asarone (Cis-Isoelemicin) may be a potential preventive drug for Alzheimer's disease. 2. Beta-Asarone prevents autophagy and synaptic loss by reducing ROCK expression in SAMP8 mice. 3. The co-administration of beta-Asarone(Cis-Isoasarone) and l-dopa may contribute to the treatment of 6-OHDA-induced damage in rats by inhibiting autophagy activity. 4. Beta-Asarone exhibits anti-inflammatory effects by suppressing the production of pro-inflammatory mediators through NF-κB signaling and the JNK pathways in activated microglial cells and might be developed as a promising candidate to treat various neuroinflammatory diseases.

Docosahexaenoic acid is an ω-3 fatty acid that is abundant in the brain and the retina and is known to be important in early development.[1] [2] Maresin 2 (MaR2) is a 13R,14S-dihydroxy DHA formed by recombinant human macrophage 12-lipoxygenase and soluble epoxide hydrolase co-incubated with DHA. [3] At 1 ng/mouse, MaR2 was shown to reduce neutrophil infiltration by 40% in a mouse model of peritonitis, and at 10 pM, MaR2 can enhance human macrophage phagocytosis of zymosan A by 90%. [3] Analytical and biological comparisons of synthetic MaR2 with endogenously derived MaR2 have confirmed its identity as matching the natural product.[4]

Gly-Gly-Phe-Gly-NH-O-CO-Exatecan is a drug-linker conjugate that integrates the linker Gly-Gly-Phe-Gly-NH-O-CO with Exatecan. This compound is essential for the formulation of antibody conjugate drugs. Exatecan acts as a DNA topoisomerase I inhibitor, which is utilized in cancer research [1] [2].

Dapagliflozin-13C6 (glucitol-13C6) is the 13C labeled compound of Dapagliflozin. Dapagliflozin has a CAS number of 461432-26-8. Dapagliflozin is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

OP-145, a derivative of the antimicrobial peptide LL-37, is a synthetic antimicrobial peptide showing activity against E. coli, P. aeruginosa, C. albicans, and A. niger, with minimum inhibitory concentrations (MICs) of 2, 3, 6, and 18 µM, respectively. Utilizing poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with OP-145 effectively prevents biofilm formation in a mouse model of bone infection, which is initiated by surgical femoral fracture and subsequent bacterial inoculation at the fracture site.

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

DTUN is a lipophilic hyponitrite radical initiator.1It initiates co-autoxidation of STY-BODIPY-embedded egg phosphatidylcholine liposomes when used at a concentration of 0.2 mM. DTUN has been used in fluorescence-enabled inhibited autoxidation (FENIX) assays for the development of ferroptosis inhibitors and the study of antioxidants in lipid membranes.1,2 1.Shah, R., Farmer, L.A., Zilka, O., et al.Beyond DPPH: Use of fluorescence-enabled inhibited autoxidation to predict oxidative cell death rescueCell Chem. Biol.26(11)1594-1607(2019) 2.Soula, M., Weber, R.A., Zilka, O., et al.Metabolic determinants of cancer cell sensitivity to canonical ferroptosis inducersNat. Chem. Biol.16(12)1351-1360(2020)

Luseogliflozin (TS 071) hydrate, a second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibits selective potency and oral activity, with an IC50 of 2.26 nM. This compound is utilized in research for the treatment of type 2 diabetes mellitus (T2DM).

Reltecimod (AB-103) TFA is an antagonist of the T-cell-specific surface glycoprotein CD28 (TP44), demonstrating efficacy against various bacterial infections, including exotoxins, endotoxins, and ionizing radiation. By modulating the inflammatory response through attenuation of the key CD28 B7-2 co-stimulatory pathway without full inhibition, Reltecimod TFA is utilized in researching necrotizing soft-tissue infections (NSTIs) [1].

COX-2-IN-14 (compound 2a) is a highly potent and selective inhibitor of COX-2 (cyclooxygenase-2), binding strongly at the active site of the COX-2 co-crystal. Demonstrating remarkable in vivo anti-inflammatory activity, COX-2-IN-14 effectively reduces ear edema and myeloperoxidase (MPO) activity in mice [1].

VUAA1, an insect odorant co-receptor (Orco) agonist, activates heteromeric and homomeric Orco-containing channels and can disrupt the behaviors of nuisance insects, thus serving as a tool for insect olfactory research [1] [2].

Tat-CIRP, a peptide inhibitor, impedes the protein-protein interaction between myeloid differentiation 2 (MD-2), also known as lymphocyte antigen 96 (LY96), and cold-inducible RNA binding protein (CIRP) by binding to MD-2. This disrupts the MD-2 and CIRP interaction as confirmed in co-immunoprecipitation assays. Notably, in vivo studies reveal that Tat-CIRP, at dosages of 10 and 20 mg/kg, significantly reduces infarct volume in both a mouse model of middle cerebral artery occlusion (MCAO) and a rhesus monkey model of thrombosis-induced stroke. Additionally, it improves motor function, evidenced by decreased time to manipulate and withdraw food with the affected arm in the primate model.

GLPG2737 is a strong CFTR type 2 corrector that can be combined with a type 1 co-corrector for cystic fibrosis research [1].

Cotransin, a Sec61 translocation inhibitor, selectively prevents the stable insertion of certain nascent chains into the Sec61 translocation channel, exhibiting signal-sequence discrimination. This compound also inhibits the expression of VCAM-1 and p-selectin proteins by blocking their co-translational translocation across endoplasmic reticulum (ER) membranes (IC 50 =0.5-5 µM). Cotransin's role extends to potential applications in inflammation and immunity research [1] [2].

Bexagliflozin (EGT1442) is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 2 nM for human SGLT2 and 5.6 μM for human SGLT1.

WYJ-2, a selective agonist for toll-like receptor 2 1 (TLR2 1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].

Leriglitazone (Hydroxypioglitazone) hydrochloride, a pioglitazone metabolite, acts as a PPARγ agonist, effectively stabilizing the PPARγ activation function-2 (AF-2) co-activator binding surface to enhance co-activator binding, which results in a modest improvement in transcriptional efficacy. It binds to the PPARγ C-terminal ligand-binding domain (LBD) with a dissociation constant (K i) of 1.2 μM and demonstrates transcriptional efficacy with an effective concentration (EC 50) of 680 nM [1].

Digalacturonic acid, a pectin or pectic acid metabolite, facilitates the co-crystallization of enzymes, including proteinase K [1] [2].

Dapagliflozin D5 (BMS-512148 D5) is a deuterated form of Dapagliflozin, a competitive SGLT2 inhibitor.