Search Result
Results for "
tissue selectivity
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12023
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GTx-007
2 Publications Verification
S-4
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Androgen Receptor
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Cancer
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GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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- HY-117658
-
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Others
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Cardiovascular Disease
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GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue .
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-
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- HY-U00178
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- HY-135732
-
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Androgen Receptor
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Cancer
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SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity .
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- HY-119433
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J867
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Progesterone Receptor
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Endocrinology
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Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human .
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-
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- HY-U00216
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-
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- HY-14210
-
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Phosphatase
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Inflammation/Immunology
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TNAP-IN-1 (Compound 1) is a selective tissue-nonspecific alkaline phosphatase (TNAP) inhibitor, with an IC50 of 0.19 μM. TNAP-IN-1 can be used for the research of soft tissue calcification .
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-
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- HY-139852
-
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Phosphatase
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Cancer
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PLAP-IN-1 is a potent (IC50 = 32 nM) and selective PLAP inhibitor, with no detectable inhibition of tissue non-specific alkaline phosphatase (TNAP) activity.
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-
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- HY-N9141
-
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5-HT Receptor
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Neurological Disease
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Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica .
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- HY-78144
-
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IAP
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Inflammation/Immunology
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4-Methylsalicylic acid is a salicylic acid. 4-Methylsalicylic acid derivative is a selective tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibitor .
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- HY-130013
-
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Fluorescent Dye
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Others
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HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
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- HY-13273
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MK-2866; GTX-024; Enobosarm
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Androgen Receptor
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Others
Cancer
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Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism .
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-
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- HY-119649
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IKI220
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Parasite
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Infection
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Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
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- HY-13556A
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LY353381 hydrochloride; SERM III hydrochloride
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Estrogen Receptor/ERR
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Cancer
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Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
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-
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- HY-115768A
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Poly-p-methoxyphenethylmethylamine (trimer)
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Others
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Others
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Compound 48/80 (trimer) is a trimer of Compound 48/80 (HY-115768). Compound 48/80 is widely used in animal and tissue models as a "selective" mast cell activator .
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-
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- HY-161835
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-
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- HY-13738A
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Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
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Estrogen Receptor/ERR
Autophagy
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Endocrinology
Cancer
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Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
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- HY-N0457A
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(-)-Chicoric acid; trans-Caffeoyltartaric acid
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HIV Integrase
HIV
Endogenous Metabolite
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Infection
Cancer
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L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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- HY-W062700
-
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Others
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Neurological Disease
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STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection .
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- HY-114056
-
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Others
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Cancer
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AS115 is a potent and selective KIAA1363 inactivator with IC50 value of 150 nM. KIAA1363 is a 2-acetyl monoacylglycerol ether (MAGE) hydrolase that is upregulated in aggressive cancers of various tissues .
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- HY-163146
-
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Fluorescent Dye
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Cancer
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TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
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- HY-P1473
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Amylin (8-37) (mouse, rat)
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Amylin Receptor
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Metabolic Disease
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Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
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- HY-131006
-
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Monoamine Transporter
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Neurological Disease
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FFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively .
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- HY-134194
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KL201
1 Publications Verification
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Cryptochrome
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Metabolic Disease
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KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .
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- HY-120017
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MD-370503
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Monoamine Oxidase
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Neurological Disease
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Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential .
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- HY-156820
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Others
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Cancer
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HLDA-221 is a heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras (RIPTACs). HLDA-221 elicits a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival, thus leading to cell death selectively in cells expressing the target protein .
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- HY-P1407
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VRPR
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MALT1
Influenza Virus
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Infection
Cancer
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Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection .
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- HY-163684
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Complement System
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Inflammation/Immunology
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Zoracopan is a selective complement factor D (CFD) inhibitor. When administered systemically (orally or intravenously), Zoracopan accumulates and is sustained-released in ocular tissues, primarily in the choroid-retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB) .
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-
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- HY-12960
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FLT3-IN-1
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FLT3
c-Kit
Apoptosis
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Cancer
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SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
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- HY-151425
-
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Others
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Cancer
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TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
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- HY-120290
-
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Histone Acetyltransferase
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Cancer
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PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity .
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- HY-147374
-
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Epigenetic Reader Domain
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Metabolic Disease
Inflammation/Immunology
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Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
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- HY-115768
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Poly-p-methoxyphenethylmethylamine
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Others
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Neurological Disease
Cancer
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Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
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- HY-150970
-
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Pyroptosis
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Cancer
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ICy-OH, an iodinated photosensitizer, is an effective anticancer agent. ICy-OH can be used not only for deep tissue imaging (λex=640 nm,λem=690-740 nm) but also to selectively induce cell death in pancreatic cancer cells via cell pyroptosis pathway .
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- HY-13738AR
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Keoxifene (hydrochloride)(Standard); LY156758(Standard); LY139481 hydrochloride (Standard)
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Estrogen Receptor/ERR
Autophagy
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Endocrinology
Cancer
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Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation?selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
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- HY-19665
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LY303870
|
Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .
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- HY-100186
-
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Androgen Receptor
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Cardiovascular Disease
Others
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
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GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
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- HY-N0457AR
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HIV Integrase
HIV
Endogenous Metabolite
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Infection
Cancer
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L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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- HY-142119
-
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mAChR
NF-κB
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Inflammation/Immunology
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Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
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- HY-120110
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IOX4
5 Publications Verification
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HIF/HIF Prolyl-Hydroxylase
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Neurological Disease
Inflammation/Immunology
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IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
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-
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- HY-W020468
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DuP 996
|
Potassium Channel
TRP Channel
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Neurological Disease
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Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue .
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- HY-137976
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Penequinine hydrochloride
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mAChR
NF-κB
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Inflammation/Immunology
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Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
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- HY-155684
-
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PROTACs
VEGFR
PDGFR
Ephrin Receptor
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Cancer
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SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .
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-
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- HY-147040
-
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c-Met/HGFR
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Cancer
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ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. ABN401 has cytotoxic activity against MET-addicted cancer cells. ABN401 can inhibit c-MET phosphorylation in tumor tissues. ABN401 can be used for researching anticancer .
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- HY-101176
-
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Melatonin Receptor
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Cancer
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2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
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-
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- HY-135747
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GR-7
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Bacterial
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Infection
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Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice .
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- HY-144126
-
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LPL Receptor
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Inflammation/Immunology
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S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
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-
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- HY-D1275
-
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Fluorescent Dye
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Others
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CAY10731 (compound 3) is a highly selective fluorescent probe for detection of hydrogen sulfide (H2S). CAY10731 is used to monitor exo- and endogenous H2S in both cancer and normal cells. CAY10731 is applied for imaging of H2S in living tissues at variable depths and in nematodes .
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- HY-103195
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NKY80
1 Publications Verification
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Adenylate Cyclase
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Metabolic Disease
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NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
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-
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- HY-131340
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
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- HY-103336
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T1117
|
GPR55
Cannabinoid Receptor
|
Cardiovascular Disease
|
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
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- HY-155685
-
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PROTACs
VEGFR
Ephrin Receptor
Apoptosis
|
Cancer
|
SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase .
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- HY-131891
-
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mAChR
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Neurological Disease
|
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
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- HY-10656
-
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Urotensin Receptor
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Inflammation/Immunology
|
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
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- HY-131334
-
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AMPK
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Metabolic Disease
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AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .
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- HY-131881
-
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mAChR
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Neurological Disease
|
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
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- HY-111056
-
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Ser/Thr Protease
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Cancer
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UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion .
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- HY-10569
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ACT-128800
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LPL Receptor
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Inflammation/Immunology
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Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-105017
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ATL 313; DE 112
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Adenosine Receptor
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Infection
Inflammation/Immunology
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Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .
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- HY-19409
-
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Calcium Channel
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Neurological Disease
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AJG049 is a novel antagonist of the Ca 2+ channel with an IC50 value of 79 nM. AJG049 can be used to reduce the contraction of intestinal smooth muscle .
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- HY-115924
-
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CDK
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Cancer
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CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
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- HY-16923A
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BIII-890 hydrochloride; BIII-890 CL
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Sodium Channel
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Neurological Disease
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Crobenetine hydrochloride (BIII-890 hydrochloride) is the hydrochloride form of Crobenetine (HY-16923). Crobenetine hydrochloride is a selective inhibitor for Na + channel. Crobenetine hydrochloride displaces 3HBTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, exhibits only low binding affinity for other receptors and ion channels. Crobenetine hydrochloride protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-19674
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SSR182289A free base
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Thrombin
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Cardiovascular Disease
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SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
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- HY-116771
-
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Adrenergic Receptor
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Metabolic Disease
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CL316243 free acid is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors. CL316243 free acid is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 free acid has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-116771A
-
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Adrenergic Receptor
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Metabolic Disease
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CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors .CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate . CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-153114
-
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FXR
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Inflammation/Immunology
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HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
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- HY-16923
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BIII-890; BIII-890 CL free acid
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Sodium Channel
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Neurological Disease
|
Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-B0639
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WR2721
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action .
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- HY-13508
-
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Histamine Receptor
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Inflammation/Immunology
|
JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .
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- HY-18572S
-
2,4-Dichlorophenoxyacetic acid-13C6
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Isotope-Labeled Compounds
DNA/RNA Synthesis
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Others
|
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
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- HY-150701
-
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Glucocorticoid Receptor
Mineralocorticoid Receptor
11β-HSD
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Metabolic Disease
|
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research .
|
-
- HY-18572S1
-
|
DNA/RNA Synthesis
|
Others
|
2,4-D-d3 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
|
-
- HY-18572S2
-
|
DNA/RNA Synthesis
|
Others
|
2,4-D-d5 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
|
-
- HY-P1821
-
MHP4-14
|
PKC
|
Neurological Disease
|
Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
|
-
- HY-B0639A
-
WR2721 trihydrate
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action .
|
-
- HY-138454
-
Mercaptoethylguanidine hemisulfate
|
NO Synthase
|
Inflammation/Immunology
|
MEG (Mercaptoethylguanidine) hemisulfate is a potent and selective inhibitor of the inducible NO synthase (iNOS), with EC50s of 11.5, 110, and 60 μM for iNOS, ecNOS, and bNOS respectively in tissue homogenates. MEG hemisulfate is also a potent scavenger of peroxynitrite and inhibits peroxynitrite-induced oxidative processes. MEG hemisulfate has a protective effect in many experimental models of inflammation, including ischemia/reperfusion injury, periodontitis, hemorrhagic shock, inflammatory bowel disease, and endotoxic and septic shock .
|
-
- HY-P1821A
-
MHP4-14 TFA
|
PKC
|
Neurological Disease
|
Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
|
-
- HY-B0561
-
SC9420
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
- HY-10569S
-
ACT-128800-d4
|
Isotope-Labeled Compounds
LPL Receptor
|
Others
|
Ponesimod-d4 (ACT-128800-d4)is the deuterium labeledPonesimod(HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-16936
-
|
LRRK2
|
Neurological Disease
|
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
|
-
- HY-136675
-
|
Others
|
Others
|
ASMI is a novel ratiometric two-photon fluorescent probe that can selectively detect and monitor mitochondrial Cys with rapid responsiveness and high contrast and brightness imaging of living cells and intact tissues at a depth of 150 μm. ASMI consists of highly two-photon active biocompatible merocyanine fluorescein and an acrylic acid group as a thiol reactive site. It has been extensively explored as a fluorescent sensing or imaging probe due to its easily tunable organelle targeting and large two-photon absorption properties. Some acrylic acid-functionalized probes tend to react more actively with Cys than with Hcy and GSH. The reaction mechanism involves the conjugate addition of Cys to acrylic acid to generate a thioether, followed by intramolecular cyclization to generate merocyanine fluorescein and a cyclic amide (Scheme 1). Importantly, the biocompatible and photostable ASMI and merocyanine show very large two-photon action cross sections (Φσmax) of 65.2 GM (λex = 740 nm) and 72.6 GM (λex = 760 nm), respectively, which make them have great potential in high-contrast and bright ratiometric two-photon excitation bioimaging applications. ASMI is a ratiometric fluorescent probe that exhibits a two-photon excitation mode for highly selective detection and imaging of mitochondrial Cys in living cells and deep tissue applications.
|
-
- HY-145801
-
|
Others
|
Inflammation/Immunology
|
XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases . XT2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P10420
-
|
CD47
Interleukin Related
|
Cancer
|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
|
-
- HY-150057
-
|
Cannabinoid Receptor
|
Others
|
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
|
-
- HY-125961
-
|
Others
|
Cancer
|
T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream) .
|
-
- HY-P99575
-
AMG-757
|
Notch
|
Inflammation/Immunology
Cancer
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
|
-
- HY-10569S1
-
ACT-128800-d7
|
Isotope-Labeled Compounds
|
Others
|
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-161449
-
|
11β-HSD
|
Metabolic Disease
|
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
|
-
- HY-108596
-
|
Potassium Channel
|
Inflammation/Immunology
|
BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) .
|
-
- HY-P3849
-
LMN-NKA
|
Neurokinin Receptor
|
Neurological Disease
|
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
|
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-117051
-
|
Others
|
Cancer
|
STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
|
-
- HY-117991
-
|
Others
|
Cancer
|
DW10075 is a novel, highly selective VEGFR inhibitor that targets the VEGF/VEGF receptor (VEGFR) pathway, which has been shown to be an effective anti-angiogenic approach for cancer therapy. Studies have found that DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3 among 21 kinases, while having no effect on the other 18 kinases, including FGFR and PDGFR. In human umbilical vein endothelial cells (HUVECs), DW10075 significantly prevented VEGF-induced activation of VEGFR and its downstream signaling, thereby inhibiting VEGF-induced HUVEC proliferation. In addition, DW10075 dose-dependently inhibited VEGF-induced HUVEC migration and tube formation, and suppressed angiogenesis in the rat aortic ring model and the chick embryo chorionic membrane model. DW10075 also exhibited antiproliferative activity against 22 different human cancer cell lines, with IC50 values ranging from 2.2 μmol/L (for U87-MG human glioblastoma cells) to 22.2 μmol/L (for A375 melanoma cells). In the nude mouse U87-MG xenograft tumor model, oral administration of DW10075 significantly inhibited tumor growth and reduced the expression of CD31 and Ki67 in tumor tissues. In summary, DW10075 is a potential anti-tumor angiogenesis agent that deserves further development.
|
-
- HY-120973
-
|
Biochemical Assay Reagents
|
Others
|
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
|
-
Cat. No. |
Product Name |
Type |
-
- HY-130013
-
|
Fluorescent Dyes/Probes
|
HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
|
-
- HY-D1275
-
|
Fluorescent Dyes/Probes
|
CAY10731 (compound 3) is a highly selective fluorescent probe for detection of hydrogen sulfide (H2S). CAY10731 is used to monitor exo- and endogenous H2S in both cancer and normal cells. CAY10731 is applied for imaging of H2S in living tissues at variable depths and in nematodes .
|
Cat. No. |
Product Name |
Type |
-
- HY-120973
-
|
Biochemical Assay Reagents
|
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1473
-
Amylin (8-37) (mouse, rat)
|
Amylin Receptor
|
Metabolic Disease
|
Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
|
-
- HY-P1407
-
VRPR
|
MALT1
Influenza Virus
|
Infection
Cancer
|
Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection .
|
-
- HY-P3849
-
LMN-NKA
|
Neurokinin Receptor
|
Neurological Disease
|
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
|
-
- HY-P10216
-
|
Peptides
|
Others
|
CAQK peptide selectively binds to injured mouse brain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
|
-
- HY-P5421
-
|
Peptides
|
Others
|
Caloxin 1B1 is a biological active peptide. (Caloxin 1b1 is obtained by screening for binding to extracellular domain 1 of PMCA4, which inhibited PMCA extracellularly, selectively, and had a higher affinity for PMCA4 than PMCA1. Because caloxin 1b1 had been selected to bind to an extracellular domain of PMCA, it could be added directly to cells and tissues to examine its effects on smooth muscle and endothelium.)
|
-
- HY-P1821
-
MHP4-14
|
PKC
|
Neurological Disease
|
Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
|
-
- HY-P10420
-
|
CD47
Interleukin Related
|
Cancer
|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99575
-
AMG-757
|
Notch
|
Inflammation/Immunology
Cancer
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-13738A
-
-
-
- HY-N0457A
-
-
-
- HY-13738AR
-
-
-
- HY-B0561
-
SC9420
|
Cardiovascular Disease
Classification of Application Fields
Disease Research Fields
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
|
-
-
- HY-P99575
-
AMG-757
|
Classification of Application Fields
Disease Research Fields
Cancer
|
Notch
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
|
-
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
-
- HY-N9141
-
-
-
- HY-N0457AR
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-18572S2
-
|
2,4-D-d5 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
|
-
-
- HY-10569S1
-
|
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
|
-
-
- HY-18572S
-
|
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
|
-
-
- HY-18572S1
-
|
2,4-D-d3 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
|
-
-
- HY-10569S
-
|
Ponesimod-d4 (ACT-128800-d4)is the deuterium labeledPonesimod(HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
|
-
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