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  • Inhibitors & Agonists
    655
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Methyldopa
MK-351, L-(-)-α-Methyldopa
T0505555-30-6
Methyldopa (MK-351), an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive medicine, is served as an antihypertensive or sympatholytic.
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Thapsigargin
TQ030267526-95-8
Thapsigargin is a natural product, an inhibitor of sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.
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1-Hydroxyanthraquinone
T37101129-43-1
1-Hydroxyanthraquinone is an anthraquinone that has been found in Morinda officinalis and has genotoxic and carcinogenic activities. 1-Hydroxyanthraquinone generates strong DNA repair response.
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Acetyl-L-carnitine hydrochloride
O-Acetyl-L-carnitine hydrochloride, O-acetyl-L-carnitine hcl, O-Acetylcarnitine hcl, Acetyl L-carnitine hydrochloride
T25635080-50-2
Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) is a nutritional supplement composed of the hydrochloride salt form of the acetylated form of the endogenously produced L-carnitine, with potential neuroprotective, cognitive-enhancing, anti-depressive and immunomodulating activities. It may also relieve peripheral neuropathy induced by chemotherapy, diabetes or other diseases. In addition, acetyl-L-carnitine may modulate the immune response by increasing T-lymphocytes maturation and may downregulate pro-inflammatory cytokines in response to viruses, such as SARS-CoV-2. It may also disrupt the ACE2 signaling pathway and inhibit the production of reactive oxygen species (ROS).
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6-Methoxyflavanone
NSC50184
TN31743034-04-6
6-Methoxyflavanone (6-MeOF) is a positive allosteric modulator of the GABA response in human recombinant GABA A receptors, exhibiting antianxiety and anti-inflammatory properties, and is used to alleviate cisplatin-induced neuropathic pain.
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Methyl palmitate
Palmitic acid methyl ester, Methyl hexadecanoate
T2S0157112-39-0
Methyl hexadecanoate is an acaricidal compound found in green walnut hulls with anti-inflammatory and antifibrotic properties, inhibiting phagocytic activity and immune response.
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Linalool
Linalol, (±)-Linalool, Phantol
T2S226478-70-6
1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.
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Sucralose
Trichlorosucrose, E955
T139956038-13-2
Sucralose is a non-nutritive artificial sweetener and sugar substitute that stimulates appetite in rodents by activating a conserved neural fasting response.
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Tacrolimus monohydrate
FK-506, FR 900506, Prograf, FR900506, Tacrolimus hydrate, LCP-Tacro, FK 506
T20879109581-93-3
Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties. It prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro and has strong immunosuppressive activity in vivo.
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Qingyangshengenin B
Otophylloside B
TMS1461106758-54-7
Qingyangshengenin B (Otophylloside B) is a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic and anti-aging effects, it can extend lifespan, increase heat stress-resistance, delay body paralysis, and increase the chemotaxis response in C. elegans models of Alzheimer's disease. Otophylloside B can suppress the seizure-like locomotor activity caused by pentylenetetrazole in zebrafish.
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Aldosterone
T1918652-39-1
Aldosterone, the primary mineralocorticoid, is synthesized and secreted by the zona glomerulosa of the adrenal cortex in response to activation of the renin-angiotensin system or high dietary potassium.
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7-10 days
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Betulonic acid
(+)-Betulonic acid, Betunolic acid, Liquidambaric acid
T5S00184481-62-3
1. Betulonic acid (Liquidambaric acid) amide stimulated the regenerative response in hepatocytes under conditions of combined toxic exposure and promoted recovery of their qualitative and quantitative characteristics, which was accompanied by a significant decrease in the severity of liver fibrosis and the absence of cirrhotic transformation of the liver. 2. Betulonic acid derivatives have a promising cytostatic activity in vitro and could be used as potential leads for the development of new type of anti-cancer agents. 3. Betulonic acid has antiholestatic effects in mice.
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Shogaol
[6]-Shogaol, 6-Shogaol
T6S1699555-66-8
1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.
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Polygalasaponin F
T3826882664-74-6
Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i
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Alliin
(S)-3-(Allylsulphinyl)-L-alanine
T5764556-27-4
Alliin ((S)-3-(Allylsulphinyl)-L-alanine) is a garlic organosulfur compound that possesses various pharmacological properties.alliin protected against LPS-induced ALI by activating PPARγ, which subsequently inhibited LPS-induced NF-κB activation and inflammatory response. Alliin might be used as an anti-inflammatory agent in the treatment of ALI.
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Retinol
Vitamin A1, Alphalin, all-trans-Retinol
T118368-26-8
Retinol (Alphalin) and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.
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Telocinobufagin
Telocinobufogenin, Telobufotoxin
T4A2462472-26-4
1. Telocinobufagin (Telobufotoxin) is the major endogenous digitalis-like factor. 2. Telocinobufagin significantly decreases the bacterial burdens in the spleen and prolongs the survival time of FIST-immunized mice challenged with live S. typhimurium. 3. Telocinobufagin has immunomodulatory activity, can enhance a Th1 immune response to control intracellular infections, could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases.
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kuwanon G
Moracenin B, Kuwanone G
T3S161275629-19-5
1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.
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2-heptyl-3-hydroxy-4(1H)-Quinolone
2-heptyl-3-hydroxy-4(1H)-Quinolone, PQS, Pseudomonas Quinolone Signal
T38373108985-27-9
2-heptyl-3-hydroxy-4(1H)-Quinolone (Pseudomonas Quinolone Signal) is a quorum-sensing signalling molecule produced by Pseudomonas aeruginosa in response to increased cell density. It increases the expression of the lasB gene in P. aeruginosa, the secretion of the metabolites pyocyanin and the lectin PA-IL, as well as increasing biofilm production in P. aeruginosa populations. It also reduces the iron content of the P. aeruginosa growth medium when used at a concentration of 40 μM and acts as an iron chelator in iron sulphate solutions.
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Atractylenolide I
T5S016773069-13-3
1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res
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Brusatol
(+)-Brusatol, NSC 172924
TQ021114907-98-3
Brusatol (NSC-172924) is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.
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Bardoxolone
RTA 401, CDDO
T2915218600-44-3
Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.
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Chlorin E6
Ce6, Chlorin e6, CE6
T3646619660-77-6
Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg kg, i.v., 50-200 J cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg m2, IV, 100 J cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.
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7-10 days
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Rosmanol
T703380225-53-2
Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce
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