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Ca2 concentration

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3

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5

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Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101396
    ICA-069673
    2 Publications Verification

    Potassium Channel Neurological Disease
    ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells .
    ICA-069673
  • HY-19044

    Potassium Channel Cardiovascular Disease
    SKF 95601 is a modulator of small conductive Ca2+-activated K+ channels with anti-atrial fibrillation (AF) activity. SKF 95601 may play a role in inhibiting atrial fibrillation by affecting the interaction between intracellular Ca2+ concentration and membrane potential. SKF 95601 has become a potential inhibitory target against atrial fibrillation due to its significant expression in various species, especially human atria .
    SKF 95601
  • HY-114743

    mAChR Histamine Receptor CRAC Channel Others
    GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high K? in guinea pig and rat tracheal smooth muscle, inhibits Ca2?-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca2?-free medium.
    GS 283
  • HY-P5319

    Others Calcium Channel Others
    MCaE12A is a high-affinity modulator of RyR2 and increases RyR2 sensitivity to cytoplasmic calcium concentrations promoting channel opening. MCaE12A acts as an important tool for RyR2 structure-to-function studies as well as for manipulating Ca2+ homeostasis and dynamic of cardiac cell .
    MCaE12A
  • HY-W010451R

    Calcium Channel Cardiovascular Disease
    1,2,4-Trihydroxybenzene (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene. This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone), a by-product of coffee bean roasting, increases intracellular Ca2+ concentration in rat thymic lymphocytes .
    1,2,4-Trihydroxybenzene (Standard)
  • HY-138035

    Fungal Infection
    Tenellin is a fungal metabolite that has been found in Beauveria. It inhibits Mg2+-, Ca2+-, and Na+/K+-ATPase activities in equine erythrocytes by 51, 57, and 74%, respectively, when used at a concentration of 200 μg/mL.1 Tenellin is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of- 4.84 and 11.95 μM, respectively.
    Tenellin
  • HY-156787

    Photofrin II

    Endogenous Metabolite Cancer
    Porfimer sodium (Photofrin II) is a photosensitizing compound used primarily for photodynamic inhibition. Porfimer sodium is selectively taken up by tumor cells and can generate oxygen free radicals upon activation. Porfimer sodium causes changes in Ca(2+) concentrations within cells, exhibiting acute electrophysiological responses and changes in cell morphology. The application of porfimer sodium can lead to the formation of micropores on the cell membrane surface, resulting in necrotic cell death .
    Porfimer sodium
  • HY-156082

    Parasite Calcium Channel Others
    RyRs activator 3 (compound A4) is an effective insecticide against diamondback moths (M. separata) and diamondback moths (P. xylostella). The LC50 value of RyRs activator 3 against diamondback moth is 3.27 mg/L. RyRs activator 3 can bind to ryanodine receptor, increase cytoplasmic Ca2+ concentration, and produce biological toxicity .
    RyRs activator 3
  • HY-12882

    RC 61-91; NP-120

    iGluR Neurological Disease
    Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
    Ifenprodil
  • HY-114252R

    Na+/K+ ATPase Cardiovascular Disease
    Strophanthidin (Standard) is the analytical standard of Strophanthidin. This product is intended for research and analytical applications. Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration .
    Strophanthidin (Standard)
  • HY-116153

    Cholinesterase (ChE) Neurological Disease
    HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2?/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
    HUHS2002
  • HY-N6789
    KT5720
    3 Publications Verification

    PKA Neurological Disease Cancer
    KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
    KT5720
  • HY-113970A

    WEB 1881 FU hydrochloride

    mAChR Neurological Disease
    Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i .
    Nebracetam hydrochloride
  • HY-D1024
    Coelenterazine h
    2 Publications Verification

    2-Deoxycoelenterazine; CLZN-h

    Calcium Channel Biochemical Assay Reagents Neurological Disease
    Coelenterazine h (2-Deoxycoelenterazine), a coelenterazine derivative, is a luminescent substrate for RLuc8. Coelenterazine h is more sensitive to Ca 2+, thus providing a valuable tool for measuring small changes in Ca 2+ concentrations .
    Coelenterazine h
  • HY-D1024A
    Coelenterazine h hydrochloride
    2 Publications Verification

    2-Deoxycoelenterazine hydrochloride; CLZN-h hydrochloride

    Biochemical Assay Reagents Calcium Channel Neurological Disease
    Coelenterazine h (2-Deoxycoelenterazine) hydrochloride, a coelenterazine derivative, is a luminescent substrate for RLuc8. Coelenterazine h hydrochloride is more sensitive to Ca 2+, thus providing a valuable tool for measuring small changes in Ca 2+ concentrations .
    Coelenterazine h hydrochloride
  • HY-W010451

    Calcium Channel Cardiovascular Disease
    1,2,4-Trihydroxybenzene (Hydroxyhydroquinone), a by-product of coffee bean roasting, increases intracellular Ca 2+ concentration in rat thymic lymphocytes .
    1,2,4-Trihydroxybenzene
  • HY-D1702

    Fluorescent Dye Others
    Mag-Fura-2 tetrapotassium is a UV excitable rational fluorescent Mg 2+/Ca 2+ indicator (Ex=334-360 nm, Em=510 nm). Mag-Fura-2 tetrapotassium can be used for the determination of Mg 2+ and Ca 2+ concentrations .
    Mag-Fura-2 tetrapotassium
  • HY-103545

    Gastric inhibitory peptide (1-39) (porcine)

    Insulin Receptor Metabolic Disease
    GIP (1-39) (Gastric inhibitory peptide (1-39) (porcine)) is an insulinotropic peptide that stimulats insulin secretion from rat pancreatic islets. GIP (1-39) at 100 nM was able to significantly increase intracellular Ca 2+ concentration ([Ca 2+]i), and capable of enhancing exocytosis .
    GIP (1-39)
  • HY-10171
    NPS-2143 hydrochloride
    15+ Cited Publications

    SB-262470A hydrochloride

    CaSR Metabolic Disease
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
    NPS-2143 hydrochloride
  • HY-10007
    NPS-2143
    15+ Cited Publications

    SB-262470A

    CaSR Metabolic Disease
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor .
    NPS-2143
  • HY-D1700

    Fluorescent Dye Others
    Mag-indo-1/AM is a cell-permeable fluorescent indicator for Mg 2+ and also for Ca 2+ (Ex=340-390 nm, Em=410-490 nm). Mag-indo-1/AM can be used to determine intracellular Mg 2+ and Ca 2+ concentrations .
    Mag-indo-1/AM
  • HY-117073

    Calcium Channel Neurological Disease
    ITH12575, a CGP37157 derivative, is a potent and selective mNCX blocker. ITH12575 reduces Ca 2+ influx through CALHM1 at low micromolar concentrations .
    ITH12575
  • HY-D0202

    Fluorescent Dye Others
    Arsenazo III is a dye useful for detection of micromolar concentrations of ionized Ca 2+. Arsenazo III can be used for determination of thorium, zirconium, uranium and rare earth elements .
    Arsenazo III
  • HY-141613A

    PKC Others
    Dioleyl phosphatidylserine is a phospholipid that can be used to form the cochlea. Dioleyl phosphatidylserine (100 μM) can activate PKC-γ under Ca 2+ concentrations < 0.5 μM .
    Dioleyl phosphatidylserine
  • HY-103306
    Ryanodine
    4 Publications Verification

    Calcium Channel Others Neurological Disease
    Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca 2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
    Ryanodine
  • HY-13103
    NS 11021
    2 Publications Verification

    Potassium Channel Others
    NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials .
    NS 11021
  • HY-P10328

    DNA/RNA Synthesis Metabolic Disease
    Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
    Vasoactive intestinal contractor
  • HY-P1076

    Calmodulin Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages .
    CALP2
  • HY-B0596S

    TA-0910-13C,d3

    Isotope-Labeled Compounds Thyroid Hormone Receptor Apoptosis Neurological Disease Endocrinology
    Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
    Taltirelin-13C,d3
  • HY-136190

    TRP Channel Neurological Disease
    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
    TRPC6-PAM-C20
  • HY-124416
    ML604086
    1 Publications Verification

    CCR Inflammation/Immunology Endocrinology
    ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations .
    ML604086
  • HY-N11887

    Reactive Oxygen Species Inflammation/Immunology
    Linocinnamarin is a nature product that could be isolated from Fragaria ananassa Duch. Linocinnamarin has anti-inflammatory activity. Linocinnamarin inhibits antigen-stimulated elevation of intracellular free Ca 2+ concentration and reactive oxygen species (ROS) .
    Linocinnamarin
  • HY-100981

    Endogenous Metabolite Neurological Disease
    MR-16728 hydrochloride is a compound that promotes the release of acetylcholine and has activity that enhances the release of acetylcholine. MR-16728 hydrochloride inhibits acetylcholine release induced by KCl depolarization. MR-16728 hydrochloride also inhibits Ca(2+)-ATPase activity in pure presynaptic membranes. The half-maximal effect of MR-16728 hydrochloride occurs at a concentration of 13.5 μM. MR-16728 hydrochloride significantly enhances the release of acetylcholine in the presence of low concentrations of calcium (approximately 10 μM range). Enhanced acetylcholine release was also observed with MR-16728 hydrochloride in proteoliposomes loaded with mediator proteins .
    MR-16728 hydrochloride
  • HY-P1076A

    Calmodulin Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages .
    CALP2 TFA
  • HY-B1837A

    beta-Cyfluthrin

    Calcium Channel Neurological Disease
    β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport .
    β-Cyfluthrin
  • HY-162501

    Piezo Channel Inflammation/Immunology
    Yaddle1 is an agonist of the mechano-activated ion channel (Piezo1) with a half-maximal effective concentration (MEC50) of 0.40 μM. Yaddle1 can significantly trigger Ca 2+ inflow in T cells and induce T cell activation response. Yaddle1 can be used in the study of vaccine adjuvants .
    Yaddle1
  • HY-114252

    Na+/K+ ATPase Cardiovascular Disease
    Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 μmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration .
    Strophanthidin
  • HY-N2500

    Microtubule/Tubulin Apoptosis Autophagy Infection Cardiovascular Disease Cancer
    Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from Anthriscus sylvestris. Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis . Deoxypodophyllotoxin induces cell autophagy and apoptosis . Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons .
    Deoxypodophyllotoxin
  • HY-N6687
    Calcimycin
    5+ Cited Publications

    A-23187; Antibiotic A-23187

    Oxidative Phosphorylation Bacterial Fungal Apoptosis Autophagy Antibiotic Infection Cancer
    Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis .
    Calcimycin
  • HY-B1837AR

    beta-Cyfluthrin (Standard)

    Calcium Channel Neurological Disease
    β-Cyfluthrin (Standard) is the analytical standard of β-Cyfluthrin. This product is intended for research and analytical applications. β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport .
    β-Cyfluthrin (Standard)
  • HY-N6687B

    A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium

    Oxidative Phosphorylation Bacterial Fungal Apoptosis Autophagy Infection Cancer
    Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces apoptosis .
    Calcimycin hemimagnesium
  • HY-117982

    GnRH Receptor ERK Endocrinology
    SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
    SKI2496
  • HY-B0596
    Taltirelin
    1 Publications Verification

    TA-0910

    Thyroid Hormone Receptor Apoptosis Neurological Disease Endocrinology
    Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
    Taltirelin
  • HY-N6687A

    A-23187 hemiCalcium salt; Antibiotic A-23187 hemiCalcium salt

    Oxidative Phosphorylation Bacterial Fungal Apoptosis Autophagy Antibiotic Infection Cancer
    Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces apoptosis .
    Calcimycin hemicalcium salt
  • HY-136409

    C10-HSL

    Bacterial Reactive Oxygen Species Infection
    N-decanoyl-L-homoserine lactone (C10-HSL) is a N-acyl-homoserine lactone (AHL) N-decanoyl-L-homoserine lactone can inhibit primary root growth in Arabidopsis. N-decanoyl-L-homoserine lactone triggers a transient and immediate increase in the concentrations of cytosolic free Ca 2+ and reactive oxygen species (ROS), increases the activity of mitogen-activated protein kinase 6 (MPK6), and induces nitric oxide (NO) production in Arabidopsis roots .
    N-Decanoyl-L-homoserine lactone
  • HY-W009724
    2-Aminoethyl diphenylborinate
    Maximum Cited Publications
    43 Publications Verification

    2-APB

    Calcium Channel TRP Channel CRAC Channel Cardiovascular Disease Inflammation/Immunology
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue .
    2-Aminoethyl diphenylborinate
  • HY-11000A

    Phosphatase Cancer
    CaMKP inhibitor sodium (compound 5) is an inhibitor of Ca 2+/neutral protein-dependent protein concentration (CaMKP) and its nuclear type (CaMKP-N) (IC50: 6.4 μM, CaMKP; 6.6 μM, CaMKP-N). CaMKP is one type of Ser/Thr protein, which can be passed through to remove the oxidized oxidized protein (CaMK). CaMKP inhibitor sodium inhibits CaMKP mediated phospho-CaMKI hydrolysis, unaffectes protein phosphoric acid 2C (PP2C) and calcineurin (CaN) .
    CaMKP inhibitor sodium
  • HY-B0596A
    Taltirelin acetate
    1 Publications Verification

    TA-0910 acetate

    Thyroid Hormone Receptor Apoptosis Neurological Disease Endocrinology
    Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
    Taltirelin acetate
  • HY-14229
    TGR5 Receptor Agonist
    2 Publications Verification

    CCDC

    G protein-coupled Bile Acid Receptor 1 Calcium Channel Metabolic Disease
    TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
    TGR5 Receptor Agonist
  • HY-B0561
    Spironolactone
    3 Publications Verification

    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 .
    Spironolactone

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