Search Result
Results for "
Calcium mobilization
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-111557
-
YM-254890
Maximum Cited Publications
17 Publications Verification
|
P2Y Receptor
|
Cardiovascular Disease
|
|
YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM .
|
-
-
- HY-P3419
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
PERK
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
|
PAMP-12 (unmodified) is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) can reduce cAMP accumulation, increase Ca 2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) can be used for the research of hypotension and ulcerative colitis .
|
-
-
- HY-B0499A
-
|
Octylonium bromide; SP63
|
mAChR
|
Neurological Disease
|
|
Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .
|
-
-
- HY-103450
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
-
- HY-P1852
-
|
|
Adenylate Cyclase
PTHR
|
Neurological Disease
|
|
TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain .
|
-
-
- HY-P0172
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
-
-
- HY-50688
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
|
-
-
- HY-P991734
-
|
|
TREM receptor
Syk
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
|
-
-
- HY-N7395
-
-
-
- HY-13628
-
|
LY293111; VML 295
|
Leukotriene Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [ 3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis .
|
-
-
- HY-124571
-
|
|
GPR84
|
Inflammation/Immunology
|
|
ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120 .
|
-
-
- HY-128121
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM) .
|
-
-
- HY-P0172A
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
-
-
- HY-N7690
-
|
|
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
-
- HY-132184
-
|
5,6-EET; (±)5,6-EpETrE
|
Adrenergic Receptor
Calcium Channel
|
Endocrinology
|
|
5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
|
-
-
- HY-110190
-
|
ML396
|
mGluR
|
Neurological Disease
|
|
VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice .
|
-
-
- HY-103138
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
|
-
-
- HY-114011
-
-
-
- HY-N0805A
-
|
|
Epoxide Hydrolase
CaMK
Autophagy
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer .
|
-
-
- HY-142117
-
|
|
Calcium Channel
Chloride Channel
|
Others
|
|
Adenophostin A is an IP3 receptor (inositol 1,4,5-trisphosphate receptors) modulator and Ca 2+ releaser, with an IC50 of 1.3 nM, an EC50 of 1.4 nM, and a Ki of 0.18 nM in rats, and an IC50 of 0.95 nM in humans. Adenophostin A activates IP3 receptors, stimulates Ca 2+ release from intracellular stores and microsomes, inhibits the binding of [ 3H]IP3 to plasma membrane receptors, and activates chloride channels. Adenophostin A resists phosphorylation and dephosphorylation by IP3 metabolic enzymes to maintain its activity, and increases cytoplasmic [Ca 2+] levels via calcium mobilization from the endoplasmic reticulum of vascular smooth muscle cells. Adenophostin A is applicable to research related to hemorrhagic shock .
|
-
-
- HY-145697
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 2 (compound 33) is a potent, selective, and orally active GPR84 antagonist (IC50=8.95 nM). GPR84 antagonist 2 shows improved potency in the calcium mobilization assay and the ability to inhibit the chemotaxis of neutrophils and macrophages upon GPR84 activation. GPR84 antagonist 2 has the potential for the research of ulcerative colitis .
|
-
-
- HY-116326
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts .
|
-
-
- HY-123763
-
|
|
CCR
|
Inflammation/Immunology
|
|
MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx .
|
-
-
- HY-147222
-
SAE-14
1 Publications Verification
GPR183 antagonist-1
|
EBI2/GPR183
|
Neurological Disease
Inflammation/Immunology
|
|
SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice .
|
-
-
- HY-145086
-
R-PSOP
1 Publications Verification
|
Neuromedin U Receptor (NMUR)
|
Metabolic Disease
|
|
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
|
-
-
- HY-172458
-
Z-3578
1 Publications Verification
|
Mas-related G-protein-coupled Receptor (MRGPR)
TNF Receptor
|
Inflammation/Immunology
|
|
Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions .
|
-
-
- HY-19434
-
|
Trans-(±)-ACP
|
mGluR
|
Metabolic Disease
|
|
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
|
-
-
- HY-N7395A
-
-
-
- HY-P2355
-
|
BOC2; Boc-Phe-dLeu-Phe-dLeu-Phe
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
BOC-FlFlF (Boc-Phe-dLeu-Phe-dLeu-Phe) is a selective FPR1 antagonist. Boc-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. Boc-FlFlF can be used for the study of inflammation .
|
-
-
- HY-134299
-
|
8-(4-Chlorophenylthio)-cAMP-AM
|
Ras
PKA
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma .
|
-
-
- HY-P3789
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Prolactin-Releasing Peptide (12-31), rat is a fragment of the prolactin releasing peptide (PrRP). Prolactin-Releasing Peptide (12-31), rat shows high affinity for GPR10 receptors. Prolactin-Releasing Peptide (12-31), stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor .
|
-
-
- HY-103138A
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .
|
-
-
- HY-117380
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
|
-
-
- HY-137325A
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
|
-
-
- HY-130704
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats .
|
-
-
- HY-167862A
-
|
|
LPL Receptor
|
Neurological Disease
|
|
UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC50 = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice .
|
-
-
- HY-177094
-
-
-
- HY-153132
-
|
|
mGluR
|
Metabolic Disease
|
|
mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC50 of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay .
|
-
-
- HY-103572
-
|
|
mGluR
|
Neurological Disease
|
|
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
|
-
-
- HY-144347
-
|
|
CXCR
|
Infection
Cancer
|
|
HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis .
|
-
-
- HY-146413
-
|
|
CXCR
HIV
|
Infection
Cancer
|
|
HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM .
|
-
-
- HY-118806A
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
|
-
-
- HY-105358
-
|
|
Leukotriene Receptor
Calcium Channel
|
Inflammation/Immunology
|
|
CP-288886 is a cysLT1 receptor antagonist with a Ki value of 0.004 μM. CP-288886 exhibits comparable activity to Zafirlukast (HY-17492) and Pranlukast (HY-B0290). CP-288886 inhibits calcium mobilization with an IC50 of 0.0005 μM in human U937 cells. CP-288886 has high oral bioavailability. CP-288886 possesses anti-asthmatic activity in a guinea pig asthma model and can be used for the research of diseases such as asthma .
|
-
-
- HY-107614G
-
|
1-Oleoyl-sn-glycero-3-phosphate sodium; 1-Oleoyl-LPA sodium
|
LPL Receptor
ROCK
TGF-beta/Smad
TGF-β Receptor
|
Neurological Disease
Cancer
|
|
1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer .
|
-
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
-
- HY-B0499AR
-
|
Octylonium bromide (Standard); SP63 (Standard)
|
Reference Standards
mAChR
|
Neurological Disease
|
|
Otilonium (bromide) (Standard) is the analytical standard of Otilonium (bromide). This product is intended for research and analytical applications. Otilonium bromide (OB) is an orally active mAChR inhibitor and smooth muscle relaxant which can interfere with the mobilization of calcium in intestinal smooth muscle, OB can be used for research of irritable bowel syndrome .
|
-
-
- HY-125313
-
|
|
Orphan GPCR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
PSB-1737 is a human-selective GPR17 agonist with an EC50 for human GPR17 of 270 nM, and its activity on murine GPR17 is relatively weak (EC50 > 10 μM). PSB-1737 shows no significant inhibition at the glycine binding site of NMDA receptors, and has no significant agonistic or antagonistic activity on P2Y receptor subtypes. PSB-1737 can be used in demyelinating diseases (such as multiple sclerosis) or inflammatory-related anemia .
|
-
-
- HY-120985
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Xestospongins and araguspongins are marine natural products first isolated from Pacific basin sponges, and noted to have vasodilatory properties.1 Inositol phosphates (IP) are important signal transduction messengers acting via IP3 receptors to promote the mobilization of Ca2+ from intracellular stores.2 Araguspongin B antagonizes the calcium-releasing action of inositol 1,4,5-trisphosphate at the receptor level in cerebral microsomes, with an IC50 of 0.6 μM. It is nearly as potent as xestospongin C as an antagonist of the IP3 receptor.
|
-
-
- HY-N7690R
-
|
|
Reference Standards
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
-
- HY-101607A
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
KT-362 free acid is an intracellular calcium antagonist with antiarrhythmic and vasodilatory effects. KT-362 free acid shows an antagonistic effect against norepinephrine (NE) induced vasoconstriction response, achieved by reducing inositol phospholipid hydrolysis, thereby reducing intracellular calcium mobilization. KT-362 free acid can be used to study the contraction and relaxation mechanisms of vascular smooth muscle, especially in exploring the role of intracellular calcium mobilization and inositol phospholipid hydrolysis in vascular contraction .
|
-
- HY-P11405
-
|
|
Neurotensin Receptor
|
Neurological Disease
Cancer
|
|
[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca 2+ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice .
|
-
![[D-Arg1,D-Trp5,7,9,Leu11]-Substance P](//file.medchemexpress.com/product_pic/hy-p11405.gif)
- HY-129808
-
|
|
LPL Receptor
|
Cardiovascular Disease
Cancer
|
|
VPC12249 is a competitive dual LPA1/LPA3 antagonist with Ki values of 137nM and 428 nM, respectively. VPC12249 inhibits calcium mobilization in HEK293T cells with a Ki value of ~130 nM. VPC12249 is promising for research of ovarian cancer and hypertensive diseases .
|
-
- HY-107216A
-
|
|
Adhesion G Protein-coupled Receptors (AGPCRs)
PI3K
|
Neurological Disease
Cancer
|
|
(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression .
|
-
- HY-165327
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
AGN-190383 is a bee venom phospholipase A2 inhibitor. AGN 190383 inhibits both hormone-operated and depolarization-dependent calcium mobilization as well as fMLP stimulated increases in free cytosolic calcium. AGN-190383 has anti-inflammatory activity .
|
-
- HY-111332
-
|
|
mGluR
|
Others
|
|
(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
|
-
- HY-125717
-
|
|
mGluR
|
Neurological Disease
|
|
VU0029251 is a mGluR5 partial antagonist (Ki: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC50: 1.7 μM) .
|
-
- HY-172321
-
|
Nicotinic acid 1,N6-ethenoadenine dinucleotide phosphate sodium
|
Fluorescent Dye
|
Others
|
|
Etheno-NAADP (Nicotinic acid 1,N6-ethenoadenine dinucleotide phosphate) sodium is a fluorescent product of NAADP (HY-103317). Etheno-NAADP sodium could activate Ca 2+ release from sea urchin egg homogenates with an EC50 of 5 µM (Ex/Em = 275/410 nm) .
|
-
- HY-174746
-
|
|
mRNA
|
Inflammation/Immunology
|
|
Human CCR2 mRNA encodes the human C-C motif chemokine receptor 2 (CCR2) protein, a chemokine which specifically mediates monocyte chemotaxis. CCR2 can mediate agonist-dependent calcium mobilization and inhibition of adenylyl cyclase.
|
-
- HY-P2355A
-
|
BOC2 TFA; Boc-Phe-dLeu-Phe-dLeu-Phe TFA
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
BOC-FlFlF (TFA) (Boc-Phe-dLeu-Phe-dLeu-Phe (TFA)) is a selective FPR1 antagonist. BOC-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. BOC-FlFlF can be used for the study of inflammation .
|
-
- HY-144784
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-144781
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM) [ 1].
|
-
- HY-144783
-
|
|
CXCR
|
Inflammation/Immunology
Cancer
|
|
CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
|
-
- HY-13628A
-
|
LY293111 sodium; VML 295 sodium
|
Leukotriene Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Etalocib (LY293111) sodium, an orally active leukotriene B4 receptor antagonist, inhibits the binding of [ 3H]LTB4, with a Ki of 25 nM. Etalocib sodium prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib sodium induces apoptosis .
|
-
- HY-118806
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
|
-
- HY-130358
-
|
|
Calcium Channel
|
Neurological Disease
|
|
PDDHV is a calcium absorption inducer and may achieve 45Ca 2+ influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
|
-
- HY-19198
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
SB-201993 is a selective leukotriene B₄ (LTB4) receptor antagonist with a Ki=7.6 nM for LTB4 receptors on human inflammatory cells. SB-201993 inhibits calcium mobilization in inflammatory cells and 5-lipoxygenase activity, exerting anti-inflammatory effects. SB-201993 is promising for research of inflammatory diseases (e.g., dermatitis, arthritis) .
|
-
- HY-13628R
-
|
LY293111 (Standard); VML 295 (Standard)
|
Leukotriene Receptor
Apoptosis
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Etalocib (Standard) is the analytical standard of Etalocib. This product is intended for research and analytical applications. Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis .
|
-
- HY-141832
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments .
|
-
- HY-N11723
-
|
Katenarin
|
CCR
CXCR
p38 MAPK
JNK
Calcium Channel
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Catenarin, an anthraquinone compound, inhibits CCR5- and CXCR4-mediated chemotaxis. Catenarin reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), and calcium mobilization. Catenarin shows anti-inflammatory effect and suppresses leukocyte migration in the diabetes. Catenarin exhibits significant inhibitory effects against Gram-positive bacteria. Catenarin prevents type 1 diabetes (T1D) in nonobese diabetic mice [1][2].
|
-
- HY-118285
-
|
|
mGluR
|
Neurological Disease
|
|
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
|
-
- HY-123357
-
|
|
Apoptosis
|
Neurological Disease
|
|
IMM-H004, a coumarin derivative, possesses neuroprotective and potent free radical scavenging abilities. IMM-H004 significantly inhibits amyloid-β (Aβ)-induced cytotoxicity and apoptosis, offering potential value for research into neurodegenerative diseases such as Alzheimer's disease. Additionally, IMM-H004 is also capable of effectively blocking the calcium mobilization and chemotaxis induced by CKLF1-C27 (HY-P3418), thereby alleviating asthmatic pathological changes in the lung tissue of CKLF1 transgenic mice .
|
-
- HY-151392
-
|
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains .
|
-
- HY-160615
-
-
- HY-P2055
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
-
- HY-116295
-
|
|
P2Y Receptor
p38 MAPK
Calcium Channel
|
Cardiovascular Disease
|
|
MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [ 35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease .
|
-
- HY-116295A
-
|
|
P2Y Receptor
p38 MAPK
Calcium Channel
|
Cardiovascular Disease
|
|
MRS2690 disodium is a selective P2Y14 receptor agonist. MRS2690 disodium inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 disodium induces intracellular calcium mobilization, activates P38 and stimulates [ 35S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690 disodium can be used for ischemic heart disease .
|
-
- HY-126638
-
|
NSC 324645
|
Parasite
|
Infection
|
|
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
|
-
- HY-N0805AR
-
|
|
Reference Standards
Epoxide Hydrolase
CaMK
Autophagy
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Alisol B (Standard) is the analytical standard of Alisol B (HY-N0805A). This product is intended for research and analytical applications. Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer.
|
-
- HY-P11259
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .
|
-
- HY-167160
-
|
|
TRP Channel
|
Neurological Disease
|
|
AZ12099548 is a TRPV1 antagonist. AZ12099548 inhibits both Capsaicin (HY-10448)- and low pH-induced calcium mobilization .
|
-
- HY-103572R
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
MNI137 (Standard) is the analytical standard of MNI137 (HY-103572). This product is intended for research and analytical applications. MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
|
-
- HY-W574030
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Fmoc-DL-Leu-OH acts as a partial agonist of the neurotensin NTS1 receptor (NTS1R) with an EC50 of 215.50 μM. Fmoc-DL-Leu-OH triggers intracellular calcium mobilization, and its activity is blocked by selective NTS1R antagonists. Fmoc-DL-Leu-OH can be used in the research of schizophrenia .
|
-
- HY-182724
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
PSB-18422 is a GPR17 agonist, with an EC50 of 0.0279 μM for humans, 0.47 μM for rats, 0.753 μM for mice, and a human Ki of 1.46 μM. PSB-18422 triggers intracellular calcium mobilization via cross-species activation of GPR17. PSB-18422 can be used in the research of allergic bronchial inflammation .
|
-
- HY-186042
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
TPα/β antagonist-1 is a TXA2 receptor α (TPα) and TPβ antagonist with IC50s of 1.52 nM and 0.79 nM, respectively. TPα/β antagonist-1 inhibits U-46619 (HY-108566)-induced intracellular calcium mobilization, and imhibits platelet aggregation. TPα/β antagonist-1 can be used for the research of cardiovascular disease .
|
-
- HY-182735
-
|
|
CCR
Cytochrome P450
5-HT Receptor
Dopamine Receptor
Serotonin Transporter
|
Inflammation/Immunology
|
|
BMS-570520 is an orally bioavailable CCR3 antagonist with an IC50 of 1.9 nM against hCCR3 and an IC50 of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis .
|
-
- HY-182587
-
|
|
mAChR
|
Neurological Disease
|
|
VU0415248 is a selective muscarinic acetylcholine receptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1 muscarinic acetylcholine receptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome .
|
-
- HY-P11769
-
|
|
CGRP Receptor
|
Cancer
|
|
RM2 is a GRPr antagonist. RM2 selectively binds to GRPr, blocks agonist-induced receptor internalization, and inhibits agonist-triggered intracellular calcium mobilization. RM2 can be used in studies related to prostate cancer .
|
-
- HY-182905
-
|
|
Somatostatin Receptor
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
|
-
- HY-N7395B
-
-
- HY-P0042
-
|
|
Somatostatin Receptor
Calcium Channel
|
Metabolic Disease
|
|
BIM-23197 is a selective SST2 (IC50 = 0.19 nM) agonist. BIM-23197 can effectively stimulate intracellular calcium mobilization in cells expressing SST2. BIM-23197 can be used for research on endocrine related conditions .
|
-
- HY-183952
-
-
- HY-182697
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
|
-
- HY-182573
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
RWJ-58259 is a selective PAR-1 inhibitor with an IC50 value of 0.15 μM. RWJ-58259 binds selectively to PAR-1, blocks the binding of tethered ligands, interferes with calcium mobilization and PAR-1-related cellular functions, and exhibits no PAR-1 agonist activity or thrombin proteolytic inhibitory activity. RWJ-58259 inhibits thrombin-induced platelet aggregation, calcium signaling and vascular smooth muscle cell proliferation, reduces neointimal thickness and arterial stenosis, and alleviates vascular occlusion and platelet deposition. RWJ-58259 can be used in the research of thrombotic diseases and vascular injury associated with acute coronary intervention .
|
-
- HY-103450R
-
|
|
Reference Standards
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G36 (Standard) is the analytical standard of G36 (HY-103450). This product is intended for research and analytical applications. G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-121621
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated .
|
-
- HY-110391
-
|
VUF 2274
|
CCR
|
Neurological Disease
Inflammation/Immunology
|
|
BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with Ki values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis .
|
-
- HY-P1650
-
|
B 9870
|
Bradykinin Receptor
ERK
|
Cancer
|
|
Breceptin (B 9870) is an antagonist of the bradykinin B1/B2 receptor (B1/B2R). Breceptin exhibits an irreversible antagonist effect on B2R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B2R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer .
|
-
- HY-P11258
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-108, a peptide compound, is a non-competitive allosteric modulator of Urotensin II receptors (UTR). UPG-108 significantly enhances the efficacy of UTR agonists but reduces the potency of UTR agonists. UPG-111 efficiently induces calcium release and does not cause contraction of rat aortic rings without endothelial denudation. UPG-111 can be used to study various diseases related to the angiotensinergic system .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-107614G
-
|
1-Oleoyl-sn-glycero-3-phosphate sodium; 1-Oleoyl-LPA sodium
|
Fluorescent Dye
|
|
1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer .
|
| Cat. No. |
Product Name |
Type |
-
- HY-107614G
-
|
1-Oleoyl-sn-glycero-3-phosphate sodium; 1-Oleoyl-LPA sodium
|
Biochemical Assay Reagents
|
|
1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3419
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
PERK
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
|
PAMP-12 (unmodified) is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) can reduce cAMP accumulation, increase Ca 2+ levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) can be used for the research of hypotension and ulcerative colitis .
|
-
- HY-P1852
-
|
|
Adenylate Cyclase
PTHR
|
Neurological Disease
|
|
TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain .
|
-
- HY-P0172
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
-
- HY-P0172A
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
|
-
- HY-P2355
-
|
BOC2; Boc-Phe-dLeu-Phe-dLeu-Phe
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
BOC-FlFlF (Boc-Phe-dLeu-Phe-dLeu-Phe) is a selective FPR1 antagonist. Boc-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. Boc-FlFlF can be used for the study of inflammation .
|
-
- HY-P3789
-
|
|
GnRH Receptor
|
Metabolic Disease
|
|
Prolactin-Releasing Peptide (12-31), rat is a fragment of the prolactin releasing peptide (PrRP). Prolactin-Releasing Peptide (12-31), rat shows high affinity for GPR10 receptors. Prolactin-Releasing Peptide (12-31), stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor .
|
-
- HY-P5756
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders .
|
-
- HY-P11405
-
|
|
Neurotensin Receptor
|
Neurological Disease
Cancer
|
|
[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca 2+ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice .
|
-
- HY-P2355A
-
|
BOC2 TFA; Boc-Phe-dLeu-Phe-dLeu-Phe TFA
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
BOC-FlFlF (TFA) (Boc-Phe-dLeu-Phe-dLeu-Phe (TFA)) is a selective FPR1 antagonist. BOC-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. BOC-FlFlF can be used for the study of inflammation .
|
-
- HY-P2055
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
-
- HY-P11259
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .
|
-
- HY-P11769
-
|
|
CGRP Receptor
|
Cancer
|
|
RM2 is a GRPr antagonist. RM2 selectively binds to GRPr, blocks agonist-induced receptor internalization, and inhibits agonist-triggered intracellular calcium mobilization. RM2 can be used in studies related to prostate cancer .
|
-
- HY-P0042
-
|
|
Somatostatin Receptor
Calcium Channel
|
Metabolic Disease
|
|
BIM-23197 is a selective SST2 (IC50 = 0.19 nM) agonist. BIM-23197 can effectively stimulate intracellular calcium mobilization in cells expressing SST2. BIM-23197 can be used for research on endocrine related conditions .
|
-
- HY-P11258
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-108, a peptide compound, is a non-competitive allosteric modulator of Urotensin II receptors (UTR). UPG-108 significantly enhances the efficacy of UTR agonists but reduces the potency of UTR agonists. UPG-111 efficiently induces calcium release and does not cause contraction of rat aortic rings without endothelial denudation. UPG-111 can be used to study various diseases related to the angiotensinergic system .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991734
-
|
|
TREM receptor
Syk
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-111557
-
-
-
- HY-N7395
-
-
-
- HY-N7690
-
|
|
Flavonoids
Classification of Application Fields
Flavones
Metabolic Disease
Plants
Disease Research Fields
Zingiberaceae
|
Calcium Channel
|
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
-
- HY-N0805A
-
|
|
Triterpenes
Structural Classification
Alisma plantago-aquatica Linn.
Classification of Application Fields
Terpenoids
Metabolic Disease
Alismataceae
Plants
Disease Research Fields
Source Classification
|
Epoxide Hydrolase
CaMK
Autophagy
Apoptosis
|
|
Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer .
|
-
-
- HY-N7395A
-
-
-
- HY-N7690R
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Zingiberaceae
|
Reference Standards
Calcium Channel
|
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
-
- HY-N11723
-
|
Katenarin
|
Quinones
Microorganisms
Anthraquinones
Source Classification
|
CCR
CXCR
p38 MAPK
JNK
Calcium Channel
|
|
Catenarin, an anthraquinone compound, inhibits CCR5- and CXCR4-mediated chemotaxis. Catenarin reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), and calcium mobilization. Catenarin shows anti-inflammatory effect and suppresses leukocyte migration in the diabetes. Catenarin exhibits significant inhibitory effects against Gram-positive bacteria. Catenarin prevents type 1 diabetes (T1D) in nonobese diabetic mice [1][2].
|
-
-
- HY-126638
-
|
NSC 324645
|
Human Gut Microbiota Metabolites
Microorganisms
Endogenous metabolite
Source Classification
|
Parasite
|
|
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC50=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.
|
-
-
- HY-N0805AR
-
|
|
Triterpenes
Structural Classification
Alisma plantago-aquatica Linn.
Terpenoids
Alismataceae
Plants
Source Classification
|
Reference Standards
Epoxide Hydrolase
CaMK
Autophagy
Apoptosis
|
|
Alisol B (Standard) is the analytical standard of Alisol B (HY-N0805A). This product is intended for research and analytical applications. Alisol B is a triterpene with diverse biological activities. Alisol B binds human soluble epoxide hydrolase (sEH) with a Ki of 5.97 μM and reduces sEH activity. Alisol B inhibits RANKL-induced JNK phosphorylation, NFATc1 and c-Fos expression, osteoclast formation, mature osteoclast pit-forming and actin ring activity, and SERCA pump activity. Alisol B induces calcium mobilization, CaMKK-AMPK-mTOR pathway activation, autophagic flux, autophagosome formation, G1 phase cell cycle arrest, endoplasmic reticulum stress, unfolded protein responses, and cancer cell apoptosis. Alisol B can be used for the research of hypercalcemia, osteoporosis, rheumatoid arthritis, periodontitis, acute kidney injury, and breast cancer.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-174746
-
|
|
|
mRNA
Chemokine & Receptors
|
|
Human CCR2 mRNA encodes the human C-C motif chemokine receptor 2 (CCR2) protein, a chemokine which specifically mediates monocyte chemotaxis. CCR2 can mediate agonist-dependent calcium mobilization and inhibition of adenylyl cyclase.
|
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-107614G
-
|
1-Oleoyl-sn-glycero-3-phosphate sodium; 1-Oleoyl-LPA sodium
|
LPL Receptor
ROCK
TGF-beta/Smad
TGF-β Receptor
|
Neurological Disease
Cancer
|
|
1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
![[D-Arg1,D-Trp5,7,9,Leu11]-Substance P](http://file.medchemexpress.com/product_pic/hy-p11405.gif)
