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PAI-1(-/-) mice

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1318

Inhibitors & Agonists

14

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16

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144

Peptides

38

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193

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4

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36

Isotope-Labeled Compounds

2

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6

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120516
    CDE-096

    		PAI-1 Cardiovascular Disease
    CDE-096 is a potent inhibitor of PAI-1. CDE-096 prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively) and is active against glycosylated PAI-1, as well as PAI-1 derived from several species (IC50=19, 22 and 18 nM for murine, rat, and Porcine PAI-1, respectively) [1].
    CDE-096
  • HY-117724
    AZ3976

    		PAI-1 Cardiovascular Disease
    AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay [1].
    AZ3976
  • HY-100447
    TM5275 sodium
    4 Publications Verification

    		 PAI-1 Cardiovascular Disease Cancer
    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
    TM5275 sodium
  • HY-15253
    Tiplaxtinin
    5+ Cited Publications

    PAI-039; Tiplasinin

    		 PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM [1].
    Tiplaxtinin
  • HY-N10227
    Geodin

    		PAI-1 Antibiotic Infection Inflammation/Immunology
    Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1) [1].
    Geodin
  • HY-122098
    Diaplasinin

    PAI-749

    		 PAI-1 Cardiovascular Disease
    Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy [1].
    Diaplasinin
  • HY-B0111
    Drospirenone

    Dihydrospirorenone

    		 Progesterone Receptor Androgen Receptor Endocrinology Cancer
    Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. [1] .
    Drospirenone
  • HY-N0518
    Toddalolactone
    1 Publications Verification

    		 PAI-1 Cardiovascular Disease
    Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM [1].
    Toddalolactone
  • HY-122714
    SK-216

    		PAI-1 Cancer
    SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma [1].
    SK-216
  • HY-106508
    Fendosal

    HP 129; P 71-0129

    		 PAI-1 Inflammation/Immunology
    Fendosal (HP 129) is an orally active, potent non-steroidal anti-inflammatory agent. Fendosal (HP 129) is also an inhibitor of Plasminogen activator inhibitor-1 (PAI-1) [1].
    Fendosal
  • HY-N1504
    Loureirin B

    		PAI-1 Potassium Channel ERK JNK Metabolic Disease
    Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
    Loureirin B
  • HY-116868
    Anecortave acetate

    Anecortave

    		 PAI-1 Cardiovascular Disease
    Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases [1] .
    Anecortave acetate
  • HY-119160
    TM5007

    		PAI-1 Inflammation/Immunology Cancer
    TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung [1].
    TM5007
  • HY-14759
    Aleplasinin

    PAZ-417

    		 PAI-1 Amyloid-β Neurological Disease
    Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research [1] .
    Aleplasinin
  • HY-101761
    TM5441
    5+ Cited Publications

    		 PAI-1 Apoptosis Cancer
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] .
    TM5441
  • HY-101761A
    TM5441 sodium

    		PAI-1 Apoptosis
    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] .
    TM5441 sodium
  • HY-120872
    AJS1669 free acid

    		Others Metabolic Disease
    AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
    AJS1669 free acid
  • HY-113878
    12-OAHSA

    		Endogenous Metabolite Metabolic Disease
    12-OAHSA is a component of olive oil. 12-OAHSA has oral activity, and improves glucose homeostasis in insulin resistant obese mice [1].
    12-OAHSA
  • HY-P5819
    xStAx-VHLL

    		Wnt APC PROTACs β-catenin Cancer
    xStAx-VHLL is a PROTAC β-catenin degrader that manifests strong inhibition of Wnt signaling and sustains degradation of β-catenin in cancer cells and the intestinal organoids derived from wild-type and APC –/– mice. xStAx-VHLL can be used as a promising anticancer agent [1].
    xStAx-VHLL
  • HY-153617
    FOXO1-IN-3

    		FOXO Metabolic Disease
    FOXO1-IN-3 is a highly-selective and orally active FOXO1 inhibitor. FOXO1-IN-3 reduces hepatic glucose production in mice. FOXO1-IN-3 improves insulin sensitivity and glucose control in db/db mice without causing weight gain [1].
    FOXO<em>1</em>-IN-3
  • HY-162396
    P-gp inhibitor 21

    		P-glycoprotein Cancer
    P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity [1].
    P-gp inhibitor 21
  • HY-126426
    CBHcy

    		DNA Methyltransferase Cardiovascular Disease
    CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model [1].
    CBHcy
  • HY-P6053
    KK-103

    		Opioid Receptor Neurological Disease
    KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect [1].
    KK-103
  • HY-110197
    6bK TFA

    		Others Metabolic Disease
    6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice [1].
    6bK TFA
  • HY-P1434
    [Pro3]-GIP (Mouse)

    		Insulin Receptor Metabolic Disease
    [Pro3]-GIP (Mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (Mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (Mouse) can be used for research of type 2 diabetes [1] .
    [Pro3]-GIP (Mouse)
  • HY-131334
    AMPK activator 4

    		AMPK Metabolic Disease
    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 [1].
    AMPK activator 4
  • HY-163087
    PT-91

    		Others Neurological Disease Metabolic Disease
    PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice [1].
    PT-91
  • HY-147548
    Keap1-Nrf2-IN-10

    		Others Others
    Keap1-Nrf2-IN-10 (compound 15) is a potent NQO1 inducer. Keap1-Nrf2-IN-10 inhibits oxidative stress by decreasing the levels of MDA, ROS, NQO1 in the liver for gamma-irradiated mice. Keap1-Nrf2-IN-10 improves the survival of gamma-irradiated mice [1].
    Keap<em>1</em>-Nrf2-IN-10
  • HY-W018723
    4-Aminobenzamidine dihydrochloride
    1 Publications Verification

    p-Aminobenzamidine dihydrochloride

    		 Ser/Thr Protease Cancer
    4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] .
    4-Aminobenzamidine dihydrochloride
  • HY-155194
    P2X7 receptor antagonist-4

    		Others Inflammation/Immunology
    P2X7 receptor antagonist-4 (Compound 14a) is a P2X7R antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC50 in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice [1].
    P2X7 receptor antagonist-4
  • HY-158311
    Anti-osteoporosis agent-8

    		RANKL/RANK p38 MAPK NF-κB Endocrinology
    Anti-osteoporosis agent-8 (Compound 4aa) is an inhibitor for RANKL, which inhibits RANKL-induced osteoclastogenesis and osteoclast differentiation (IC50 is 2.41 μM) in cells RAW264.7. Anti-osteoporosis agent-8 ameliorates bone loss in an ovariectomized (OVX) mice model [1].
    Anti-osteoporosis agent-8
  • HY-157430
    BET-IN-21

    		Epigenetic Reader Domain Neurological Disease
    BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice [1].
    BET-IN-21
  • HY-100827
    Safotibant

    LF22-0542

    		 Bradykinin Receptor Inflammation/Immunology
    Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model [1] .
    Safotibant
  • HY-N10171
    GB-2a

    		Others Inflammation/Immunology
    GB-2a is a bioflavonoids that can be isolated from Rheedia gardneriana. GB-2a has significant analgesic activity in mice with 58.9% inhibition [1].
    GB-2a
  • HY-160025
    IDO antagonist-1

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO antagonist-1 (compound 163) is an antagonist of IDO . IDO antagonist-1 inhibits pancreatic adenocarcinoma cells growth in C57BL/6 mice [1].
    IDO antagonist-<em>1</em>
  • HY-147529
    mGluR2 modulator 3

    		mGluR Neurological Disease
    mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice [1].
    mGluR2 modulator 3
  • HY-P4885
    Glp-amyloid-β (3-40) peptide (human)

    AβpE3-40

    		 Amyloid-β Neurological Disease
    Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice [1].
    Glp-amyloid-β (3-40) peptide (human)
  • HY-149357
    Yhhu6669

    		HBV Infection
    Yhhu6669 is an anti-HBV agent. Yhhu6669 inhibits HBV DNA. Yhhu6669 inhibits HBV replication by inducing the formation of DNA-free capsids. Yhhu6669 decreases HBV DNA and HBcAg in AAV/HBV-infected mice. Yhhu6669 has favorable PK properties [1].
    Yhhu6669
  • HY-120589
    VU0360172

    		mGluR Neurological Disease
    VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice [1]. VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    VU0360172
  • HY-161372
    PARP1/c-Met-IN-1

    		PARP c-Met/HGFR Apoptosis Cancer
    PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice [1].
    PARP<em>1</em>/c-Met-IN-<em>1</em>
  • HY-100426A
    Osemozotan hydrochloride

    MKC242

    		 5-HT Receptor Neurological Disease
    Osemozotan hydrochloride (MKC242) is a selective 5-HT1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder [1] .
    Osemozotan hydrochloride
  • HY-156276
    SP4e

    		PPAR Metabolic Disease
    SP4e is an activator of PPAR-γ, with the EC50 of 739 nM in HK-2 cells. SP4e reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice [1].
    SP4e
  • HY-156277
    SP4f

    		PPAR Metabolic Disease
    SP4f is an activator ofPPAR-γ, with the EC50 of 826 nM in HK-2 cells. SP4f reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice [1].
    SP4f
  • HY-161471
    DCLK1-IN-5

    		Ser/Thr Protease Inflammation/Immunology
    DCLK1-IN-5 (Compound a24) is a DCLK1 inhibitor (IC50: 179.7 nM). DCLK1-IN-5 inhibits lipopolysaccharide (HY-D1056)-induced inflammation via inhibiting DCLK1-mediated IKKβ phosphorylation. DCLK1-IN-5 protects mice against inflammation-induced lung injury and sepsis [1].
    DCLK<em>1</em>-IN-5
  • HY-P3248
    J5 peptide

    Myelin basic protein (85-99) antagonist

    		 Biochemical Assay Reagents Inflammation/Immunology
    J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases [1].
    J5 peptide
  • HY-122964
    URB447

    		Cannabinoid Receptor Metabolic Disease
    URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity [1].
    URB447
  • HY-149874
    BMS-502

    		DGK Inflammation/Immunology
    BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research [1].
    BMS-502
  • HY-146496
    Antitubercular agent-20

    		Bacterial Infection
    Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice [1].
    Antitubercular agent-20
  • HY-125527A
    17(R)-Resolvin D1

    17(R)-RvD1; AT-RvD1

    		 TRP Channel Inflammation/Immunology
    17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells [1]. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
    17(R)-Resolvin D<em>1</em>
  • HY-146495
    Antitubercular agent-19

    		Bacterial Infection
    Antitubercular agent-19 (Compound 1c) is an antitubercular agent. Antitubercular agent-19 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-19 shows low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice [1].
    Antitubercular agent-19

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