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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
35 Results for "
human wild-type receptor
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "human wild-type receptor" in MCE Product Catalog:
11
11 Publications Verification
Cat. No.: HY-16985
CAS No.: 1297538-32-9
Synonyms: ODM-201; BAY-1841788
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Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
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6 Cited Publications
Synonyms: GDC-9545; RG6171
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Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER + breast cancer .
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6 Cited Publications
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Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
1
1 Cited Publications
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GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM .
Cat. No.: HY-P99384
CAS No.: 1312305-12-6
Synonyms: B-701; MFGR-1877S; RG-7444
Cat. No.: HY-W010162
CAS No.: 1948-31-8
Synonyms: L-Alanyl-L-alanine; Ala-Ala
Cat. No.: HY-P5506
CAS No.: 144555-23-7
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Cat. No.: HY-N0475
CAS No.: 74285-86-2
Synonyms: Hypolide; (+)-Triptophenolide
Cat. No.: HY-162735
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BRD5080 is a GPR65 agonist. BRD5080 activates GPR65 to enhance the cAMP signaling pathway, reduce the expression of inflammatory cytokines and chemokines in dendritic cells, enhance the activity of human wild-type, mouse wild-type, and human GPR65 I231L variant receptors in a pH-dependent manner, and mediate the recruitment of Gαs protein. BRD5080 can be used in the research of inflammatory bowel disease .
Cat. No.: HY-16985S
CAS No.: 2484757-20-0
Synonyms: ODM-201-d4; BAY-1841788-d4
Cat. No.: HY-P4776
CAS No.: 202463-00-1
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Cat. No.: HY-16985R
CAS No.: 1297538-32-9
Synonyms: ODM-201 (Standard); BAY-1841788 (Standard)
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Research Areas:
Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
Cat. No.: HY-118806A
CAS No.: 447407-36-5
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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 .
Cat. No.: HY-148777
CAS No.: 2682255-44-1
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A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer .
Cat. No.: HY-103320
CAS No.: 652973-93-8
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Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
Cat. No.: HY-135903
CAS No.: 2407529-33-1
Synonyms: GDC-9545 tartrate; RG6171 tartrate
Target:
Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC50 of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1 Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1 Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER + breast cancer .
Cat. No.: HY-118806
CAS No.: 244291-63-2
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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 .
Cat. No.: HY-171906
CAS No.: 65446-08-4
Synonyms: 1-Arachidonoyl-sn-glycerol 3-phosphate; 1-Arachidonoyl LPA; LPA (20:4)
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1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin; HY-130567) . 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM . It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS . It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate .
Cat. No.: HY-N0475R
CAS No.: 74285-86-2
Synonyms: Hypolide (Standard); (+)-Triptophenolide (Standard)
Cat. No.: HY-168384
CAS No.: 875158-73-9
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M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
