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Results for "

pA2

" in MedChemExpress (MCE) Product Catalog:

82

Inhibitors & Agonists

1

Biochemical Assay Reagents

14

Peptides

4

Recombinant Proteins

6

Isotope-Labeled Compounds

4

Antibodies

4

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0693
    Ranitidine
    3 Publications Verification

    Histamine Receptor Metabolic Disease Cancer
    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice [2].
    Ranitidine
  • HY-10349
    WAY-100635
    Maximum Cited Publications
    12 Publications Verification

    5-HT Receptor Dopamine Receptor Neurological Disease
    WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist [2] .
    WAY-100635
  • HY-B0281A
    Ranitidine hydrochloride
    3 Publications Verification

    Histamine Receptor Metabolic Disease Cancer
    Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice [2].
    Ranitidine hydrochloride
  • HY-15895
    Aprocitentan
    3 Publications Verification

    ACT-132577

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
    Aprocitentan
  • HY-76569
    Desfesoterodine
    1 Publications Verification

    PNU-200577; 5-Hydroxymethyl Tolterodine

    mAChR Neurological Disease Cancer
    Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [2] . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
    Desfesoterodine
  • HY-107647
    (S)-(+)-Dimethindene maleate
    1 Publications Verification

    mAChR Histamine Receptor Inflammation/Immunology
    (S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
    (S)-(+)-Dimethindene maleate
  • HY-15010
    L-371,257
    1 Publications Verification

    Oxytocin Receptor Vasopressin Receptor Cardiovascular Disease Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) [2].
    L-371,257
  • HY-108626

    NCGC84

    Neuropeptide S Receptor Neurological Disease
    ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively [2].
    ML154
  • HY-15895S

    ACT-132577-d4

    Isotope-Labeled Compounds Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
    Aprocitentan-d4
  • HY-101189

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity [2].
    JNJ-39758979
  • HY-101336

    RS-17053

    Adrenergic Receptor Metabolic Disease Endocrinology
    RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
    RS 17053 hydrochloride
  • HY-17351

    RO 610612

    Endothelin Receptor Cardiovascular Disease Neurological Disease Endocrinology Cancer
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
    Tezosentan
  • HY-101232
    Tiotidine
    2 Publications Verification

    ICI 125211

    Histamine Receptor Cardiovascular Disease
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors [2].
    Tiotidine
  • HY-P2026

    Natriuretic Peptide Receptor (NPR) Cardiovascular Disease
    A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
    A 71915
  • HY-101308A
    MRS2179 tetrasodium hydrate
    2 Publications Verification

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors [2]. MRS2179 tetrasodium hydrate inhibits platelet aggregation .
    MRS2179 tetrasodium hydrate
  • HY-108562

    Prostaglandin Receptor Neurological Disease
    SC-51322 is a potent and selective antagonist of prostaglandin E2 (PGE2) receptor (EP 1), with a pA2 of 8.1. SC-51322 has the pain-relieving effect .
    SC-51322
  • HY-P1143A

    GCGR Metabolic Disease
    [Des-His1,Glu9]-Glucagon amide TFA is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide TFA is potentially useful in the study of the pathogenesis of diabetes .
    [Des-His1,Glu9]-Glucagon amide TFA
  • HY-103428
    LE 300
    2 Publications Verification

    Dopamine Receptor 5-HT Receptor Neurological Disease
    LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay [2].
    LE 300
  • HY-P1143

    GCGR Metabolic Disease
    [Des-His1,Glu9]-Glucagon amide is a potent and peptide antagonist of the glucagon receptor, with a pA2 of 7.2. [Des-His1,Glu9]-Glucagon amide is potentially useful in the study of the pathogenesis of diabetes .
    [Des-His1,Glu9]-Glucagon amide
  • HY-151413
    MEN 10207
    1 Publications Verification

    Neurokinin Receptor Neurological Disease
    MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
    MEN 10207
  • HY-P10473A

    Neuromedin U Receptor (NMUR) Inflammation/Immunology
    CPN-351 TFA (compound 9a), a pentapeptide, is a selective antagonist of human NMUR1 with a pA2 of 7.35. The antagonistic effect of CPN-351 TFA on human NMUR1 is 10 times higher than that on NMUR2. CPN-351 TFA can be used in the study of inflammation . X
    CPN-351 TFA
  • HY-103135

    5-HT Receptor Neurological Disease
    SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT2B / 5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92) . SB 206553 possesses anxiolytic-like properties [2].
    SB 206553 hydrochloride
  • HY-B0693A

    Histamine Receptor SARS-CoV Bacterial Infection Metabolic Disease Cancer
    Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice [2] .
    Ranitidine bismuth citrate
  • HY-P11091

    Bacterial Infection
    PA2-GNU7 is an antimicrobial peptide (AMP). PA2-GNU7 exhibits potent antimicrobial activity with minimal inhibitory concentration (MIC) against P. aeruginosa, E. coli, S. typhimurium, S. aureus, and C. albicans are 2 μM, 1 μM, 2 μM, 2 μM, and 8 μM, respectively. PA2-GNU7 rapidly and selectively kills Pseudomonas aeruginosa without affecting other commensal bacteria. PA2-GNU7 significantly improves survival of mice infected with P. aeruginosa. PA2-GNU7 can be used for the research and development of therapeutic agents against MDR Pseudomonas aeruginosa infections .
    PA2-GNU7
  • HY-144377

    RAR/RXR Neurological Disease Metabolic Disease Cancer
    RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research .
    RXR antagonist 1
  • HY-P10473

    Neuromedin U Receptor (NMUR) Inflammation/Immunology
    CPN-351 (compound 9a), a pentapeptide, is a selective antagonist of human NMUR1 with a pA2 of 7.35. The antagonistic effect of CPN-351 on human NMUR1 is 10 times higher than that on NMUR2. CPN-351 can be used in the study of inflammation .
    CPN-351
  • HY-19432

    iGluR Neurological Disease
    UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96 [2].
    UBP-282
  • HY-14782

    SLV313

    5-HT Receptor Dopamine Receptor Neurological Disease
    Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics .
    Adoprazine
  • HY-P3850

    Neurokinin Receptor Neurological Disease
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A .
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
  • HY-16979

    Opioid Receptor Neurological Disease
    RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects .
    TRK-851
  • HY-101308

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors [2]. MRS2179 tetrasodium inhibits platelet aggregation .
    MRS2179 tetrasodium
  • HY-P1320

    Opioid Receptor Inflammation/Immunology
    [Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
    [Nphe1]Nociceptin(1-13)NH2
  • HY-76569R

    PNU-200577 (Standard); 5-Hydroxymethyl Tolterodine (Standard)

    Reference Standards mAChR Neurological Disease
    Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [2] . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
    Desfesoterodine (Standard)
  • HY-170601

    PROTACs JNK Cancer
    PROTAC JNK1-targeted-1 (PA2) is a JNK1 PROTAC degrader, with a DC50 of 10 nM. PROTAC JNK1-targeted-1 (PA2) decreases the level of Fibronectin protein. PROTAC JNK1-targeted-1 can be used for the research of pulmonary fibrosis . (Pink: JNK1 inhibitor (HY-170602); Black: linker (HY-40178); Blue: CRBN Ligand (HY-41547))
    PROTAC JNK1-targeted-1
  • HY-105483

    Leukotriene Receptor Inflammation/Immunology
    MDL 43291 is a competitive leukotriene (LT) receptor antagonist. MDL 43291 antagonize LTD4 and LTE4 with pA2 of 6.7. MDL 43291 does not antagonize histamine, carbachol or substance P. MDL 43291 can be used for the researches of inflammation and immunology, such as asthma .
    MDL 43291
  • HY-15895R

    ACT-132577 (Standard)

    Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .
    Aprocitentan (Standard)
  • HY-P5006

    d(CH2)5[Tyr(Me)2, Dab5]AVP

    Vasopressin Receptor Cardiovascular Disease
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP) is a specific antagonist of vasopressin V1a receptor, with a pA2 of 6.71 .
    (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin
  • HY-10382

    Angiotensin Receptor Cardiovascular Disease
    EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA2 value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research .
    EXP-6803
  • HY-P11442

    Lycotoxin-pA2a; TBIU041425

    Bacterial Toll-like Receptor (TLR) Inflammation/Immunology
    Lytx-Pa2a (Lycotoxin-Pa2a) is a peptide inhibitor against bacterial membranes and TLR4 receptor. Lytx-Pa2a exerts antimicrobial effects via non-competitive disruption of outer/cytoplasmic membranes and suppression of LPS-induced TLR4/NF-κB signaling. Lytx-Pa2a is promising for research of bacterial infection and inflammation-related disease (e.g., sepsis) .
    Lytx-Pa2a
  • HY-100152

    SX 810

    mAChR Inflammation/Immunology
    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.
    Beperidium iodide
  • HY-121603

    Cholinesterase (ChE) Neurological Disease
    Bornaprine is an anticholinergic agent that can be used in the study of parkinsonism. Bornaprine shows a pA2 value of 7.27 .
    Bornaprine
  • HY-P1017

    Neurokinin Receptor Cardiovascular Disease Neurological Disease
    MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66 .
    MDL 29913
  • HY-76569S1

    PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14

    mAChR Isotope-Labeled Compounds Neurological Disease
    (R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [2] . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
    (R)-Hydroxytolterodine-d14
  • HY-139045

    5-HT Receptor Neurological Disease
    2,4-DMA hydrochloride is an amphetamine and is a serotonin 5-HT2 receptor agonist with an apparent PA2 value of 5.6 .
    2,4-DMA hydrochloride
  • HY-U00355

    YM-57158

    Leukotriene Receptor Prostaglandin Receptor Inflammation/Immunology Endocrinology
    YM158 free base is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.
    YM158 free base
  • HY-W713312

    5-HT Receptor Neurological Disease
    2,6-DMA hydrochloride is classified as an amphetamine. 2,6-DMA hydrochloride is a serotonin 5-HT2 receptor agonist with an apparent pA2 value of 5.09.
    2,6-DMA hydrochloride
  • HY-19136

    5-HT Receptor Neurological Disease
    WAY-100289 is an orally active antagonist for 5-HT3 receptor, that exhibits high affinity to the isolated rat vagus nerves with pA2 of 8.9. WAY-100289 inhibits the Bezold-Jarisch reflex in anesthetized and awake rats .
    WAY-100289
  • HY-14757

    SL-650472

    5-HT Receptor Neurological Disease
    Trelanserin (SL-650472) is a 5-HT receptor antagonist and also an effective in vitro smooth muscle contraction antagonist, competing against the contractions induced by sumatriptan (HY-B0121B) with a pA2 of 8.17±0.36 .
    Trelanserin
  • HY-119262

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence [2].
    ABT-866
  • HY-170474

    2,N,N-TMT; 2-Me-DMT

    5-HT Receptor Neurological Disease
    2-Methyl-N,N-dimethyltryptamine (2,N,N-TMT, compound 15) has binding affinity for serotonin (5-HT) receptor, with the pA2 of 6.04. 2-Methyl-N,N-dimethyltryptamine plays an important role in neurological disease research .
    2-Methyl-N,N-dimethyltryptamine

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